HDAC
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1047 | Vorinostat (SAHA) | <1 mg/mL | 52 mg/mL | ''3 mg/mL |
| S1053 | Entinostat (MS-275) | <1 mg/mL | 75 mg/mL | <1 mg/mL |
| S1030 | Panobinostat (LBH589) | <1 mg/mL | 69 mg/mL | <1 mg/mL |
| S1045 | Trichostatin A (TSA) | <1 mg/mL | 23 mg/mL | ''''<1 mg/mL |
| S1122 | Mocetinostat (MGCD0103) | <1 mg/mL | 13 mg/mL | <1 mg/mL |
| S3592 | 4-Phenylbutyric acid (4-PBA) | <1 mg/mL | 33 mg/mL | ''33 mg/mL |
| S0864 | ACY-775 | <1 mg/mL | 66 mg/mL | '''66 mg/mL |
| S1313 | GSK3117391 | <1 mg/mL | 81 mg/mL | 15 mg/mL |
| S8962 | BRD3308 | <1 mg/mL | 57 mg/mL | <1 mg/mL |
| S0709 | Tubastatin A TFA | 5 mg/mL | 40 mg/mL | <1 mg/mL |
| S1085 | Belinostat (PXD101) | <1 mg/mL | 64 mg/mL | <1 mg/mL |
| S3020 | Romidepsin (FK228, Depsipeptide) | <1 mg/mL | 10 mg/mL | ''<1 mg/mL |
| S1484 | MC1568 | <1 mg/mL | 13 mg/mL | <1 mg/mL |
| S2627 | Tubastatin A HCl | <1 mg/mL | 74 mg/mL | '<1 mg/mL |
| S2170 | Givinostat (ITF2357) | <1 mg/mL | 95 mg/mL | '3 mg/mL |
| S1095 | Dacinostat (LAQ824) | <1 mg/mL | 76 mg/mL | <1 mg/mL |
| S1194 | CUDC-101 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S1096 | Quisinostat (JNJ-26481585) 2HCl | <1 mg/mL | 79 mg/mL | <1 mg/mL |
| S1515 | Pracinostat (SB939) | <1 mg/mL | 72 mg/mL | 27 mg/mL |
| S2012 | PCI-34051 | <1 mg/mL | 59 mg/mL | <1 mg/mL |
| S1422 | Droxinostat | <1 mg/mL | 49 mg/mL | 49 mg/mL |
| S1090 | Abexinostat (PCI-24781) | <1 mg/mL | 80 mg/mL | <1 mg/mL |
| S7229 | RGFP966 | <1 mg/mL | 72 mg/mL | <1 mg/mL |
| S2244 | AR-42 | <1 mg/mL | 63 mg/mL | 63 mg/mL |
| S8001 | Ricolinostat (ACY-1215) | <1 mg/mL | 86 mg/mL | <1 mg/mL |
| S1168 | Valproic acid sodium salt (Sodium valproate) | 33 mg/mL | 33 mg/mL | 33 mg/mL |
| S2818 | Tacedinaline (CI994) | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S2759 | Fimepinostat (CUDC-907) | <1 mg/mL | 102 mg/mL | <1 mg/mL |
| S1999 | Sodium butyrate | 22 mg/mL | <1 mg/mL | '22 mg/mL |
| S1848 | Curcumin | <1 mg/mL | 73 mg/mL | '<1 mg/mL |
| S2779 | M344 | <1 mg/mL | 62 mg/mL | 4 mg/mL |
| S2239 | Tubacin | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7292 | RG2833 (RGFP109) | <1 mg/mL | 68 mg/mL | 10 mg/mL |
| S2693 | Resminostat | <1 mg/mL | 70 mg/mL | '70 mg/mL |
| S1703 | Divalproex Sodium | 62 mg/mL | 62 mg/mL | 62 mg/mL |
| S8043 | Scriptaid | <1 mg/mL | 65 mg/mL | <1 mg/mL |
| S4125 | Sodium Phenylbutyrate | 30 mg/mL | 8 mg/mL | <1 mg/mL |
| S8049 | Tubastatin A | <1 mg/mL | 67 mg/mL | '<1 mg/mL |
| S3981 | Sinapinic Acid | <1 mg/mL | 44 mg/mL | 44 mg/mL |
| S7324 | TMP269 | <1 mg/mL | 100 mg/mL | 2 mg/mL |
| S7595 | Santacruzamate A (CAY10683) | <1 mg/mL | 55 mg/mL | 55 mg/mL |
| S8502 | TMP195 | <1 mg/mL | 91 mg/mL | 91 mg/mL |
| S5810 | UF010 | <1 mg/mL | 54 mg/mL | 54 mg/mL |
| S7617 | Tasquinimod | <1 mg/mL | 81 mg/mL | 11 mg/mL |
| S8743 | SKLB-23bb | <1 mg/mL | 79 mg/mL | 79 mg/mL |
| S9275 | Isoguanosine | -1 mg/mL | 57 mg/mL | -1 mg/mL |
| S6548 | NKL 22 | <1 mg/mL | 65 mg/mL | 3 mg/mL |
| S7726 | BRD73954 | <1 mg/mL | 56 mg/mL | 9 mg/mL |
| S8464 | Citarinostat (ACY-241) | <1 mg/mL | 41 mg/mL | '93 mg/mL |
| S5905 | Suberohydroxamic acid | 4 mg/mL | 41 mg/mL | '<1 mg/mL |
| S7593 | Splitomicin | <1 mg/mL | 39 mg/mL | 39 mg/mL |
| S7278 | HPOB | <1 mg/mL | 62 mg/mL | 38 mg/mL |
| S7569 | LMK-235 | <1 mg/mL | 58 mg/mL | 58 mg/mL |
| S5438 | Biphenyl-4-sulfonyl chloride | -1 mg/mL | 50 mg/mL | -1 mg/mL |
| S7473 | Nexturastat A | <1 mg/mL | 68 mg/mL | 2 mg/mL |
| S1073 | BML-210 (CAY10433) | <1 mg/mL | 68 mg/mL | 3 mg/mL |
| S6738 | TC-H 106 | <1 mg/mL | 68 mg/mL | '2 mg/mL |
| S2132 | SR-4370 | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S8773 | TH34 | <1 mg/mL | 51 mg/mL | 15 mg/mL |
| S8567 | Tucidinostat (Chidamide) | <1 mg/mL | 78 mg/mL | 2 mg/mL |
| S6687 | SIS17 | <1 mg/mL | 73 mg/mL | 18 mg/mL |
| S2341 | (-)-Parthenolide | <1 mg/mL | 49 mg/mL | 49 mg/mL |
| S8495 | WT161 | <1 mg/mL | 86 mg/mL | 1 mg/mL |
| S7596 | CAY10603 | <1 mg/mL | 89 mg/mL | '5 mg/mL |
| S8648 | ACY-738 | <1 mg/mL | 54 mg/mL | 1 mg/mL |
| S9262 | Raddeanin A | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S8769 | Tinostamustine(EDO-S101) | <1 mg/mL | 14 mg/mL | 2 mg/mL |
| S7555 | Domatinostat (4SC-202) | <1 mg/mL | 89 mg/mL | ''<1 mg/mL |
| S7689 | BG45 | <1 mg/mL | 42 mg/mL | 2 mg/mL |
| S8323 | ITSA-1 (ITSA1) | <1 mg/mL | 58 mg/mL | 5 mg/mL |
亜型選択性的な製品
HDAC製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1047 |
Vorinostat (SAHA)Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification. |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
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| S1053 |
Entinostat (MS-275)Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3. |
(A) U87 cells were cultured in the presence of DMSO, 1 uM MS-275 alone, 100 ng/ml IFN-λ1 alone, or both for the course of 4 d. Cell numbers were manually determined by hemacytometer counting at the indicated time points. (B, F) Cell proliferation of U87 cells or U87 spheroids in 3D culture with indicated treatment were performed using the WST-1 assay, which measures active cellular metabolism. (C) U87 spheroid formation in 3D culture was photographed at day 14 in culture (representative images are shown; 200x magnification). (D-E) Quantification of the relative sizes and numbers of U87 spheroids in (C). (G) Cell cycle analysis was performed in U87 cells with indicated treatment using propidium iodide staining. Numbers in the histogram show fractions (percent) of sub-G1, N, 2N, and polyploidy from left to right. (H) U87 cells with indicated treatment were stained with Annexin V-FITC and 7-AAD. Numbers indicate the percentage of FITC-positive cells (upper left quadrant). FITC, fluorescein isothiocyanate; 7-AAD, 7-Aminoactinomycin. In all panels, data represent the mean and SEM of at least three experiments.
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| S1030 |
Panobinostat (LBH589)Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3. |
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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| S1045 |
Trichostatin A (TSA)Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays. |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h, and their expression of GRP78, PERK-eIF2α axis and ATF4, ATF3, CHOP and DR5 proteins. |
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| S1122 |
Mocetinostat (MGCD0103)Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2. |
Comparison of MCAS ovarian cancer cells harboring control and CtBP2 knockdown shRNAs for sensitivity to chemotherapeutic agents. For each cell line, the MTT reading of the untreated cells was assigned as 100%. HDAC inhibitors: (a) Trichostatin A; (b) Vorinostat; (c) Belinostat; (d) MGCD0103; (e) valproic acid; and (f ) carboplatin, a non-HDAC inhibitor. |
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| S3592新 |
4-Phenylbutyric acid (4-PBA)4-Phenylbutyric acid (4-PBA, Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models. |
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| S0864新 |
ACY-775ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5 nM. |
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| S1313新 |
GSK3117391GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor. |
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| S8962新 |
BRD3308BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. |
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| S0709新 |
Tubastatin A TFATubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
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| S1085 |
Belinostat (PXD101)Belinostat (PXD101, NSC726630, PX-105684) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy. |
Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h. |
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| S3020 |
Romidepsin (FK228, Depsipeptide)Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells. |
Effects of combination of bort/romidepsin on HDAC6 inhibition and activation of ER stress signaling. HA cells were treated with combination of 15 nM bortezomib and 5 nM romidepsin or either drug alone for 24 hr. Expression of CHOP/GADD153 (green signals) and cleaved PARP (red signals) was detected by immunofluorescent staining. DAPI (blue signals) stained the cell nuclei. |
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| S1484 |
MC1568MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM in a cell-free assay. It is 34-fold more selective for HD1-A than HD1-B. |
HDAC4 and OA1 expression correlate inversely during starvation, and HDAC4 inhibition or knockdown leads to OA1 transgene up-regulation. Quantification of OA1 mRNA expression by real-time PCR in HeLa-OA1myc cells at the indicated times of incubation with MC1568 (class II HDACi). Data are expressed as the fold change compared with the amount of the OA1 mRNA in mock conditions at each time point. |
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| S2627 |
Tubastatin A HClTubastatin A HCl (TSA) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S2170 |
Givinostat (ITF2357)Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2. |
Cells were treated with indicated HDAC inhibitors for 4 days and then cultured without drug for an additional 4 days. On day 8, HDAC inhibitors were added back to the culture for another 4 days. The percentage of GFP-positive cells was measured at days 4, 8 and 12. The concentrations of HDAC inhibitors used for the experiments are as follows: vorinostat, 1 uM; TsA, 200 nM; oxamflatin, 1 uM; scriptaid, 1 uM; belinostat, 200 nM; and givinostat, 200 nM. The fraction of GFP-positive cells was measured by flow cytometry at the indicated timepoints. The effect of HDAC inhibitors or anti-CD3 plus anti-CD28 antibodies over time was normalized to the effect of anti-CD3 plus anti-CD28 antibodies at day 2. Error bars represent SEM, n = 3. APHA, 3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxypropenamide.
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| S1095 |
Dacinostat (LAQ824)Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter. |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S1194 |
CUDC-101CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). *, P < 0.05; **, P < 0.01.
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| S1096 |
Quisinostat (JNJ-26481585) 2HClQuisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2. |
WT ESCs were treated with varying concentrations of the HDAC1 specific inhibitor JNJ-26481585 for 24 h. Lysates were collected for ChIP experiments, and a H3K27ac antibody was used for immunoprecipitation (IP). qPCR was performed using primers specific for Hoxa1 RARE2. ChIP with an IgG antibody (negative control) is included in each panel. Error bars represent standard error of independent experiments where n = 3 for biological repeats. *, p < 0.05.
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| S1515 |
Pracinostat (SB939)Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2. |
Hyperacetylation of P. falciparum proteins by SB939. Synchronous 3D7 trophozoite-stage P. falciparum parasites were treated with 50 or 500 nM chloroquine (CQ), SAHA, or SB939 or with vehicle only (control; 0.05% DMSO) for 3 h. Following saponin lysis, parasite protein lysates were prepared and SDS-PAGE and Western blotting carried out using anti-acetyl H4 or anti-pan-acetyl lysine (K103) antibodies. Coomassie blue staining was carried out as a loading control.
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| S2012 |
PCI-34051PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis. |
(d) Effects of HDAC8 activity on ISO-induced augmentation of apoptosis and TIPRL expression. H1299 cells were sequentially treated with 10 μm PCI-34051 for 24 h, ISO for 30 min and 50 μM cisplatin for 48 h before the western blot analysis.
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| S1422 |
DroxinostatDroxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10. |
Chemical inhibition of HDAC3, -6, and -8 with the selective HDAC inhibitor Droxinostat (2 uM) resulted in a significant increase in the percent of 2D10 cells expressing GFP in cells that had been depleted of HDAC3 but not HDAC1 or -2. (*p<0.05).
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| S1090 |
Abexinostat (PCI-24781)Abexinostat (PCI-24781, CRA-024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2. |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S7229 |
RGFP966RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC. |
THP-1 cells were treated with indicated concentrations of Ara-C and/or RGFP966 for 24 h, and lysates were immunoblotted for p-AKT473, AKT and γH2AX.
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| S2244 |
AR-42AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1. |
One- to 2-month-old mice of both genotypes showed an increase in H3K4me3 (n = 5 to 6 per group) associated with a dose-dependent increase in neurogenesis in Kmt2d+/βGeo mice (monitored by normalized DCX expression) (n = 4 to 6 per group) upon treatment with the HDACi AR-42. There was no difference in either H3K4me3 or neurogenesis between Kmt2d+/βGeo and Kmt2d+/+ animals at a dose of 10 mg/kg per day.
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| S8001 |
Ricolinostat (ACY-1215)Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2. |
(a) Representative images from hTERT RPE-1 cells transiently transfected with siControl (siC), treated with vehicle (DMSO), alisertib (MLN8237) or rocilinostat (ACY1215) at the time of serum withdrawal for 48 h. Ciliation monitored by immunofluorescent staining using acetylated α-tubulin (cilia marker) and pericentrin (basal body marker). Nuclei counterstained using DAPI. Highlighted boxes show magnified cilia. Scale bar, 3 μM. |
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| S1168 |
Valproic acid sodium salt (Sodium valproate)Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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| S2818 |
Tacedinaline (CI994)Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3. |
A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and -actin.
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| S2759 |
Fimepinostat (CUDC-907)CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
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| S1999 |
Sodium butyrateSodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells. |
U87 cells were cultured with DMSO or 10 µM 5azadC for 72 h. For the latter, 1 µM Trichostatin A (TSA), 10 mM sodium butyrate (NaBu), 5 mM nicotinamide (NAM), or 0.5 µM apicidin were added in the last 24 h. IFNLR1 expression was determined by RT-qPCR. |
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| S1848 |
CurcuminCurcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM）and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
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| S2779 |
M344M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation. |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h. ATF4, ATF3, CHOP and DR5 proteins were measured by Western blot. |
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| S2239 |
TubacinTubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis. |
Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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| S7292 |
RG2833 (RGFP109)RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively. |
The cells were treated with 1 μM RG2833 (HDAC1/3 inhibitor), 2 μM RGFP966 (HDAC3 inhibitor), 1 μM TSA (pan-HDAC inhibitor), or vehicle for 16 h in serum-free medium. Cell lysates were analysed by Western blotting for expression of SREBP-2 activated fragment, HMG-CoA reductase and APP. Shown are representative blots and quantifications with means ± SEM of the indicated number of independent experiments performed in duplicate. *p < 0.05; **p < 0.01; n.s., not significant in one-sample t-test.
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| S2693 |
ResminostatResminostat (RAS2410) dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM. |
Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
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| S1703 |
Divalproex SodiumDivalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy. |
Divalproex sodium increases the level of acetylated histone H3 level in ataxin-3-transfected HEK293 cells. Normal (15CAG) or expanded (77CAG) ataxin-3-transfected cells were treated with divalproex sodium (Selleck chemical, 0.3 mmol/L in DMSO, (+)) or with DMSO alone (−) 48 h after transfection. The cells were treated with divalproex sodium or DMSO over 6, 12, and 24 h. The Western blot was probed with antiacetylated histone H3, antihistone H3, and antiataxin-3. Antibodies include antihistone H3 and antiataxin-3 are used as controls. The x-axis shows the different treatment group. The y-axis represents the acetylated histone H3 values normalized to histone H3. Error bars represent the standard error of the mean. Data represent three independent experiments (n = 3). The data with a normal distribution were analyzed with Student’s t-test. *P < 0.05
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| S8043 |
ScriptaidScriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3. |
The relative expression of Oct4, Nanog, Klf4 and Sox2 at the blastocyst stage in ICSI-, ROSI- and ROSI + incubation of zygotes with 250 nM Scriptaid for 10 h (ROSI-S)-derived embryos. Five blastocysts in each pool were examined to obtain the data set in each column. Q-PCR analysis was performed in triplicate. Different letters indicate significant differences between values (P < 0.05).
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| S4125 |
Sodium PhenylbutyrateSodium phenylbutyrate is a salt of 4-phenylbutyrate (4-PBA) or 4-phenylbutyric acid.Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders. |
Representative images and quantitative analysis results of the transwell experiment. Notes: (A) Results of migration assay for DU145. (B) Results of invasion assay for DU145. (C) Results of migration assay for PC3. (D) Results of invasion assay for PC3. “*” Means significantly different from control group, P<0.05. Abbreviation: SPB, sodium phenylbutyrate.
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| S8049 |
Tubastatin ATubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S3981 |
Sinapinic AcidSinapinic acid (Sinapic acid) is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) acts as an inhibitor of HDAC, with IC50 of 2.27 mM, and also inhibits ACE-I activity. |
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| S7324 |
TMP269TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
Staining of live (calcein-AM, green) and dead (PI, red) UCC cells after 72 h of treatment with TMP269. Data shown are a representative experiment of a set of 3
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| S7595 |
Santacruzamate A (CAY10683)Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs. |
Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
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| S8502 |
TMP195TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays. |
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| S3944 |
Valproic acid (VPA)Valproic acid (VPA, 2-Propylvaleric Acid, Sodium valproate) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling. |
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| S5810 |
UF010UF010 is a class I HDAC-selective inhibitor with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM and 15.3 nM for HDAC1, HDAC2, HDAC3, HDAC8, HDAC6 and HDAC10, respectively. |
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| S7617 |
TasquinimodTasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3. |
Western blot images suggested inhibition of HDAC4 increased the expression of NOX4 and MMP-9, and treatment with 10 μM SCM-198 reduced the raised levels of NOX4 and MMP-9. |
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| S8743 |
SKLB-23bbSKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. |
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| S9275 |
IsoguanosineIsoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML.Isoguanosine is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium. |
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| S6548 |
NKL 22NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM. |
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| S5771 |
SulforaphaneSulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis. |
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| S7726 |
BRD73954BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively. |
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| S8464 |
Citarinostat (ACY-241)Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. |
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| S5905 |
Suberohydroxamic acidSuberohydroxamic acid (suberic bishydroxamic acid) is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively. |
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| S7593 |
SplitomicinSplitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay. |
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| S7278 |
HPOBHPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs. |
Effects of HPOB on GCs-induced apoptosis in PC12 and SH-SY5Y cells. (A) Effect of 48 h treatment with HPOB alone and (B) anti-apoptotic effect of HPOB pre-treatment for 24 h on Cort-induced apoptosis in PC12 cells. The results are expressed as the means ± SD of three independent experiments. ## indicates a significant difference from the control (P < 0.01). * indicates a significant difference from treatment with Cort alone at P < 0.05. ** indicates a significant difference from treatment with Cort alone at P < 0.01.
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| S7569 |
LMK-235LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively. |
Upper panel: qPCR analysis of CDX2-negative HT29 cells treated with increasing concentrations of the DNMTi decitabine (1.25 μM, 2.5 μM, 5 μM, 10 μM) for 48 h and increasing concentrations of the HDAC4/5i LMK-235 (5 nM, 10 nM, 20 nM, 40 nM, 80 nM). Data were normalized to the HMBS housekeeping gene and are shown as n-fold regulation compared with DMSO-treated cells. MWU: ***p < 0.001, (n = 4). Lower panel: CDX2 Western blot analysis of the three highest concentrations for both compounds of HT29 cells treated as above. Total protein is shown as a loading control. Percentage indicates amount of protein normalized to respective DMSO controls
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| S5438 |
Biphenyl-4-sulfonyl chlorideBiphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. |
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| S7473 |
Nexturastat ANexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs. |
HDAC inhibitors disrupt SS18-SSX/TLE1 co-localization. A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells. |
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| S1073 |
BML-210 (CAY10433)BML-210 (CAY10433) is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM. |
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| S6738 |
TC-H 106TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively. |
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| S2132 |
SR-4370SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. |
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| S8773 |
TH34TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM). |
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| S8567 |
Tucidinostat (Chidamide)Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. |
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| S6687 |
SIS17SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. |
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| S2341 |
(-)-Parthenolide(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions. |
-Parthenolide-S234101W0220161110.gif)
-Parthenolide-S234101W0220161110.gif)
G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells |
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| S8495 |
WT161WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis. |
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| S7596 |
CAY10603CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs. |
U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
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| S8648 |
ACY-738ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs. |
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| S9262 |
Raddeanin ARaddeanin A (Raddeanin R3, NSC382873), a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity. |
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| S8769 |
Tinostamustine(EDO-S101)Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs). |
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| S7555 |
Domatinostat (4SC-202)Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. |
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| S7689 |
BG45BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. |
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| S8323 |
ITSA-1 (ITSA1)ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1047 |
Vorinostat (SAHA)Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification. |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
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| S1053 |
Entinostat (MS-275)Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3. |
(A) U87 cells were cultured in the presence of DMSO, 1 uM MS-275 alone, 100 ng/ml IFN-λ1 alone, or both for the course of 4 d. Cell numbers were manually determined by hemacytometer counting at the indicated time points. (B, F) Cell proliferation of U87 cells or U87 spheroids in 3D culture with indicated treatment were performed using the WST-1 assay, which measures active cellular metabolism. (C) U87 spheroid formation in 3D culture was photographed at day 14 in culture (representative images are shown; 200x magnification). (D-E) Quantification of the relative sizes and numbers of U87 spheroids in (C). (G) Cell cycle analysis was performed in U87 cells with indicated treatment using propidium iodide staining. Numbers in the histogram show fractions (percent) of sub-G1, N, 2N, and polyploidy from left to right. (H) U87 cells with indicated treatment were stained with Annexin V-FITC and 7-AAD. Numbers indicate the percentage of FITC-positive cells (upper left quadrant). FITC, fluorescein isothiocyanate; 7-AAD, 7-Aminoactinomycin. In all panels, data represent the mean and SEM of at least three experiments.
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| S1030 |
Panobinostat (LBH589)Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3. |
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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| S1045 |
Trichostatin A (TSA)Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays. |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h, and their expression of GRP78, PERK-eIF2α axis and ATF4, ATF3, CHOP and DR5 proteins. |
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| S1122 |
Mocetinostat (MGCD0103)Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2. |
Comparison of MCAS ovarian cancer cells harboring control and CtBP2 knockdown shRNAs for sensitivity to chemotherapeutic agents. For each cell line, the MTT reading of the untreated cells was assigned as 100%. HDAC inhibitors: (a) Trichostatin A; (b) Vorinostat; (c) Belinostat; (d) MGCD0103; (e) valproic acid; and (f ) carboplatin, a non-HDAC inhibitor. |
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| S3592新 |
4-Phenylbutyric acid (4-PBA)4-Phenylbutyric acid (4-PBA, Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models. |
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| S0864新 |
ACY-775ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5 nM. |
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| S1313新 |
GSK3117391GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor. |
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| S8962新 |
BRD3308BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. |
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| S0709新 |
Tubastatin A TFATubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
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| S1085 |
Belinostat (PXD101)Belinostat (PXD101, NSC726630, PX-105684) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy. |
Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h. |
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| S3020 |
Romidepsin (FK228, Depsipeptide)Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells. |
Effects of combination of bort/romidepsin on HDAC6 inhibition and activation of ER stress signaling. HA cells were treated with combination of 15 nM bortezomib and 5 nM romidepsin or either drug alone for 24 hr. Expression of CHOP/GADD153 (green signals) and cleaved PARP (red signals) was detected by immunofluorescent staining. DAPI (blue signals) stained the cell nuclei. |
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| S1484 |
MC1568MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM in a cell-free assay. It is 34-fold more selective for HD1-A than HD1-B. |
HDAC4 and OA1 expression correlate inversely during starvation, and HDAC4 inhibition or knockdown leads to OA1 transgene up-regulation. Quantification of OA1 mRNA expression by real-time PCR in HeLa-OA1myc cells at the indicated times of incubation with MC1568 (class II HDACi). Data are expressed as the fold change compared with the amount of the OA1 mRNA in mock conditions at each time point. |
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| S2627 |
Tubastatin A HClTubastatin A HCl (TSA) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S2170 |
Givinostat (ITF2357)Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2. |
Cells were treated with indicated HDAC inhibitors for 4 days and then cultured without drug for an additional 4 days. On day 8, HDAC inhibitors were added back to the culture for another 4 days. The percentage of GFP-positive cells was measured at days 4, 8 and 12. The concentrations of HDAC inhibitors used for the experiments are as follows: vorinostat, 1 uM; TsA, 200 nM; oxamflatin, 1 uM; scriptaid, 1 uM; belinostat, 200 nM; and givinostat, 200 nM. The fraction of GFP-positive cells was measured by flow cytometry at the indicated timepoints. The effect of HDAC inhibitors or anti-CD3 plus anti-CD28 antibodies over time was normalized to the effect of anti-CD3 plus anti-CD28 antibodies at day 2. Error bars represent SEM, n = 3. APHA, 3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxypropenamide.
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| S1095 |
Dacinostat (LAQ824)Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter. |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S1194 |
CUDC-101CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). *, P < 0.05; **, P < 0.01.
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| S1096 |
Quisinostat (JNJ-26481585) 2HClQuisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2. |
WT ESCs were treated with varying concentrations of the HDAC1 specific inhibitor JNJ-26481585 for 24 h. Lysates were collected for ChIP experiments, and a H3K27ac antibody was used for immunoprecipitation (IP). qPCR was performed using primers specific for Hoxa1 RARE2. ChIP with an IgG antibody (negative control) is included in each panel. Error bars represent standard error of independent experiments where n = 3 for biological repeats. *, p < 0.05.
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| S1515 |
Pracinostat (SB939)Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2. |
Hyperacetylation of P. falciparum proteins by SB939. Synchronous 3D7 trophozoite-stage P. falciparum parasites were treated with 50 or 500 nM chloroquine (CQ), SAHA, or SB939 or with vehicle only (control; 0.05% DMSO) for 3 h. Following saponin lysis, parasite protein lysates were prepared and SDS-PAGE and Western blotting carried out using anti-acetyl H4 or anti-pan-acetyl lysine (K103) antibodies. Coomassie blue staining was carried out as a loading control.
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| S2012 |
PCI-34051PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis. |
(d) Effects of HDAC8 activity on ISO-induced augmentation of apoptosis and TIPRL expression. H1299 cells were sequentially treated with 10 μm PCI-34051 for 24 h, ISO for 30 min and 50 μM cisplatin for 48 h before the western blot analysis.
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| S1422 |
DroxinostatDroxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10. |
Chemical inhibition of HDAC3, -6, and -8 with the selective HDAC inhibitor Droxinostat (2 uM) resulted in a significant increase in the percent of 2D10 cells expressing GFP in cells that had been depleted of HDAC3 but not HDAC1 or -2. (*p<0.05).
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| S1090 |
Abexinostat (PCI-24781)Abexinostat (PCI-24781, CRA-024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2. |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S7229 |
RGFP966RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC. |
THP-1 cells were treated with indicated concentrations of Ara-C and/or RGFP966 for 24 h, and lysates were immunoblotted for p-AKT473, AKT and γH2AX.
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| S2244 |
AR-42AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1. |
One- to 2-month-old mice of both genotypes showed an increase in H3K4me3 (n = 5 to 6 per group) associated with a dose-dependent increase in neurogenesis in Kmt2d+/βGeo mice (monitored by normalized DCX expression) (n = 4 to 6 per group) upon treatment with the HDACi AR-42. There was no difference in either H3K4me3 or neurogenesis between Kmt2d+/βGeo and Kmt2d+/+ animals at a dose of 10 mg/kg per day.
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| S8001 |
Ricolinostat (ACY-1215)Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2. |
(a) Representative images from hTERT RPE-1 cells transiently transfected with siControl (siC), treated with vehicle (DMSO), alisertib (MLN8237) or rocilinostat (ACY1215) at the time of serum withdrawal for 48 h. Ciliation monitored by immunofluorescent staining using acetylated α-tubulin (cilia marker) and pericentrin (basal body marker). Nuclei counterstained using DAPI. Highlighted boxes show magnified cilia. Scale bar, 3 μM. |
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| S1168 |
Valproic acid sodium salt (Sodium valproate)Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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| S2818 |
Tacedinaline (CI994)Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3. |
A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and -actin.
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| S2759 |
Fimepinostat (CUDC-907)CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
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| S1999 |
Sodium butyrateSodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells. |
U87 cells were cultured with DMSO or 10 µM 5azadC for 72 h. For the latter, 1 µM Trichostatin A (TSA), 10 mM sodium butyrate (NaBu), 5 mM nicotinamide (NAM), or 0.5 µM apicidin were added in the last 24 h. IFNLR1 expression was determined by RT-qPCR. |
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| S1848 |
CurcuminCurcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM）and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
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| S2779 |
M344M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation. |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h. ATF4, ATF3, CHOP and DR5 proteins were measured by Western blot. |
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| S2239 |
TubacinTubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis. |
Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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| S7292 |
RG2833 (RGFP109)RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively. |
The cells were treated with 1 μM RG2833 (HDAC1/3 inhibitor), 2 μM RGFP966 (HDAC3 inhibitor), 1 μM TSA (pan-HDAC inhibitor), or vehicle for 16 h in serum-free medium. Cell lysates were analysed by Western blotting for expression of SREBP-2 activated fragment, HMG-CoA reductase and APP. Shown are representative blots and quantifications with means ± SEM of the indicated number of independent experiments performed in duplicate. *p < 0.05; **p < 0.01; n.s., not significant in one-sample t-test.
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| S2693 |
ResminostatResminostat (RAS2410) dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM. |
Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
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| S1703 |
Divalproex SodiumDivalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy. |
Divalproex sodium increases the level of acetylated histone H3 level in ataxin-3-transfected HEK293 cells. Normal (15CAG) or expanded (77CAG) ataxin-3-transfected cells were treated with divalproex sodium (Selleck chemical, 0.3 mmol/L in DMSO, (+)) or with DMSO alone (−) 48 h after transfection. The cells were treated with divalproex sodium or DMSO over 6, 12, and 24 h. The Western blot was probed with antiacetylated histone H3, antihistone H3, and antiataxin-3. Antibodies include antihistone H3 and antiataxin-3 are used as controls. The x-axis shows the different treatment group. The y-axis represents the acetylated histone H3 values normalized to histone H3. Error bars represent the standard error of the mean. Data represent three independent experiments (n = 3). The data with a normal distribution were analyzed with Student’s t-test. *P < 0.05
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| S8043 |
ScriptaidScriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3. |
The relative expression of Oct4, Nanog, Klf4 and Sox2 at the blastocyst stage in ICSI-, ROSI- and ROSI + incubation of zygotes with 250 nM Scriptaid for 10 h (ROSI-S)-derived embryos. Five blastocysts in each pool were examined to obtain the data set in each column. Q-PCR analysis was performed in triplicate. Different letters indicate significant differences between values (P < 0.05).
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| S4125 |
Sodium PhenylbutyrateSodium phenylbutyrate is a salt of 4-phenylbutyrate (4-PBA) or 4-phenylbutyric acid.Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders. |
Representative images and quantitative analysis results of the transwell experiment. Notes: (A) Results of migration assay for DU145. (B) Results of invasion assay for DU145. (C) Results of migration assay for PC3. (D) Results of invasion assay for PC3. “*” Means significantly different from control group, P<0.05. Abbreviation: SPB, sodium phenylbutyrate.
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| S8049 |
Tubastatin ATubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S3981 |
Sinapinic AcidSinapinic acid (Sinapic acid) is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) acts as an inhibitor of HDAC, with IC50 of 2.27 mM, and also inhibits ACE-I activity. |
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| S7324 |
TMP269TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
Staining of live (calcein-AM, green) and dead (PI, red) UCC cells after 72 h of treatment with TMP269. Data shown are a representative experiment of a set of 3
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| S7595 |
Santacruzamate A (CAY10683)Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs. |
Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
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| S8502 |
TMP195TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays. |
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| S3944 |
Valproic acid (VPA)Valproic acid (VPA, 2-Propylvaleric Acid, Sodium valproate) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling. |
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| S5810 |
UF010UF010 is a class I HDAC-selective inhibitor with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM and 15.3 nM for HDAC1, HDAC2, HDAC3, HDAC8, HDAC6 and HDAC10, respectively. |
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| S7617 |
TasquinimodTasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3. |
Western blot images suggested inhibition of HDAC4 increased the expression of NOX4 and MMP-9, and treatment with 10 μM SCM-198 reduced the raised levels of NOX4 and MMP-9. |
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| S8743 |
SKLB-23bbSKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. |
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| S9275 |
IsoguanosineIsoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML.Isoguanosine is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium. |
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| S6548 |
NKL 22NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM. |
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| S5771 |
SulforaphaneSulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis. |
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| S7726 |
BRD73954BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively. |
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| S8464 |
Citarinostat (ACY-241)Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. |
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| S5905 |
Suberohydroxamic acidSuberohydroxamic acid (suberic bishydroxamic acid) is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively. |
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| S7593 |
SplitomicinSplitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay. |
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| S7278 |
HPOBHPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs. |
Effects of HPOB on GCs-induced apoptosis in PC12 and SH-SY5Y cells. (A) Effect of 48 h treatment with HPOB alone and (B) anti-apoptotic effect of HPOB pre-treatment for 24 h on Cort-induced apoptosis in PC12 cells. The results are expressed as the means ± SD of three independent experiments. ## indicates a significant difference from the control (P < 0.01). * indicates a significant difference from treatment with Cort alone at P < 0.05. ** indicates a significant difference from treatment with Cort alone at P < 0.01.
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| S7569 |
LMK-235LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively. |
Upper panel: qPCR analysis of CDX2-negative HT29 cells treated with increasing concentrations of the DNMTi decitabine (1.25 μM, 2.5 μM, 5 μM, 10 μM) for 48 h and increasing concentrations of the HDAC4/5i LMK-235 (5 nM, 10 nM, 20 nM, 40 nM, 80 nM). Data were normalized to the HMBS housekeeping gene and are shown as n-fold regulation compared with DMSO-treated cells. MWU: ***p < 0.001, (n = 4). Lower panel: CDX2 Western blot analysis of the three highest concentrations for both compounds of HT29 cells treated as above. Total protein is shown as a loading control. Percentage indicates amount of protein normalized to respective DMSO controls
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| S5438 |
Biphenyl-4-sulfonyl chlorideBiphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. |
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| S7473 |
Nexturastat ANexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs. |
HDAC inhibitors disrupt SS18-SSX/TLE1 co-localization. A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells. |
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| S1073 |
BML-210 (CAY10433)BML-210 (CAY10433) is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM. |
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| S6738 |
TC-H 106TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively. |
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| S2132 |
SR-4370SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. |
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| S8773 |
TH34TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM). |
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| S8567 |
Tucidinostat (Chidamide)Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. |
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| S6687 |
SIS17SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. |
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| S2341 |
(-)-Parthenolide(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions. |
-Parthenolide-S234101W0220161110.gif)
-Parthenolide-S234101W0220161110.gif)
G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells |
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| S8495 |
WT161WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis. |
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| S7596 |
CAY10603CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs. |
U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
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| S8648 |
ACY-738ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs. |
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| S9262 |
Raddeanin ARaddeanin A (Raddeanin R3, NSC382873), a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity. |
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| S8769 |
Tinostamustine(EDO-S101)Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs). |
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| S7555 |
Domatinostat (4SC-202)Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. |
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| S7689 |
BG45BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S8323 |
ITSA-1 (ITSA1)ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors. |
2021, 13(1):7 2018, 78(20):5731-5740 |
