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)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1047	Vorinostat (SAHA, MK0683)	<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
S8773	TH34	<1 mg/mL	51 mg/mL	15 mg/mL
S5810	UF010	<1 mg/mL	54 mg/mL	54 mg/mL
S5905	Suberohydroxamic acid	4 mg/mL	41 mg/mL	<1 mg/mL
S9262	Raddeanin A	-1 mg/mL	100 mg/mL	-1 mg/mL
S5438	Biphenyl-4-sulfonyl chloride	-1 mg/mL	50 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	Rocilinostat (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	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
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
S7617	Tasquinimod	<1 mg/mL	81 mg/mL	11 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
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
S7473	Nexturastat A	<1 mg/mL	68 mg/mL	2 mg/mL
S8567	Tucidinostat (Chidamide)	<1 mg/mL	78 mg/mL	2 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
S7555	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

All (57) HDAC阻害剤(56) HDAC活性剤(1) 新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, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.	Nature, 2011, 471(7337):235-9 Nature, 2017, 551(7679):247-250 Nat Biotechnol, 2011, 29(3):255-65	Activity of vorinostat in Jurkat and Peer T-ALL cell lines in an MTT cell viability assay. Cells were treated with increasing drug concentrations for 72 h. The data are plotted as the mean % of DMSO-treated control cells against the corresponding drug concentration. The error bars are the standard error. For each drug and cell line, 3-4 independent experiments were performed with 6 replicates at each drug concentration.
S1053	Entinostat (MS-275) Entinostat (MS-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. Phase 3.	Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130 Nat Immunol, 2014, 15(5):439-48	(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.
S1030	Panobinostat (LBH589) Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.	Nat Biotechnol, 2011, 29(3):255-65 Nat Med, 2015, 10.1038/nm.3855 Cell, 2018, 173(6):1413-1425	(G) A375 parental and BRAFi-resistant ex vivo clones were treated with a panel of HDACi (1 μM vorinostat, 0.5 μM belinostat, and 6 nM panobinostat) in single treatment or in combination with 1 μM vemurafenib in a long-term colony formation assay.
S1045	Trichostatin A (TSA) Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.	Nature, 2017, 551(7679):247-250 Nat Biotechnol, 2015, 10.1038/nbt.3130 Cell, 2017, 171(4):824-835.e18	Gck expression in WT primary hepatocytes transduced with FOXO1 and KR-FOXO1 adenoviruses in the presence or absence of trichostatinA (TSA).
S1122	Mocetinostat (MGCD0103) Mocetinostat (MGCD0103) 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. Phase 2.	Nat Biotechnol, 2015, 10.1038/nbt.3130 Circ Res, 2012, 110(5):739-48 Blood, 2014, 123(10):1535-43	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.
S8773^新	TH34 TH34 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).
S5810^新	UF010 UF010 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.
S5905^新	Suberohydroxamic acid Suberohydroxamic acid is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively.
S9262^新	Raddeanin A Raddeanin A, a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity.
S5438^新	Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
S1085	Belinostat (PXD101) Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.	Nat Biotechnol, 2011, 29(3):255-65 Cell, 2018, 173(6):1413-1425 Clin Cancer Res, 2017, 23(12):3139-3149	A375DR and parental cells were seeded 50,000 cells per well in 6-well plates and treated with 1 mMvorinostat (Vor), 0.5 mMbelinostat (Bel), 5 nMpanobinostat (Pan), and/or combination of 5 nM trametinib and 0.125 mM dabrafenib.
S3020	Romidepsin (FK228, Depsipeptide) Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.	Nature, 2017, 551(7679):247-250 Blood, 2018, 131(4):397-407 Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384	Concentration over time for each dose cohort of romidepsin (B).
S1484	MC1568 MC1568 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.	Nat Commun, 2013, 4:2735 Proc Natl Acad Sci USA, 2012, 109(34):E2284-93 Diabetes, 2013, 63(2):645-54	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.
S2627	Tubastatin A HCl Tubastatin A HCl 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).	Int J Cancer, 2013, 134(11):2560-71 J Med Chem, 2015, 58(2):785-800 J Biol Chem, 2013, 288(20):14400-7	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.
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.	PLoS Pathog, 2014, 10(4):e1004071 Diabetologia, 2018, 61(2):389-398 J Neurosci, 2013, 33(17):7535-47	(e–h) Cytokine secretion. Pancreatic islets were isolated from 12-week (wk)-old non-diabetic, untreated diabetic or givinostat (Givi)-treated diabetic NOD-huCD3ε mice (after 3–4 weeks of treatment) (n = 5–9 per group). Islets were cultured at 37°C for 48 h and supernatant fractions were collected. Concentrations of (e) IL-1β, (f) IL-6, (g) TNF-α and (h) IL-10 were determined by ELISA; *p < 0.05.
S1095	Dacinostat (LAQ824) Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.	Nat Biotechnol, 2011, 29(3):255-65 Diabetologia, 2012, 55(9):2421-31 Cell Physiol Biochem, 2017, 41(3):1255-1266	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.
S1194	CUDC-101 CUDC-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.	J Chem Inf Model, 2014, 54(3):881-93 ACS Med Chem Lett, 2013, 4(9):858-62 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	(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.
S1096	Quisinostat (JNJ-26481585) 2HCl Quisinostat (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.	J Clin Oncol, 2016, 10.1200/JCO.2016.66.5547 Nat Commun, 2015, 6:8648 Nat Commun, 2013, 4:2735	In vitro drug sensitivity of (C) quisinostat. Acute lymphoblastic leukemia cell lines (NALM-6, KOPN-30bi) and primary cultured cells established from patient 21 were cultured with the indicated concentrations of anticancer drugs, and viability was measured at 48 hours. Data are presented as percentages of dimethylsulfoxide (DMSO) control and depict the mean 6 standard deviation.
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. Phase 2.	PLoS Pathog, 2014, 10(4):e1004071 Antimicrob Agents Chemother, 2012, 56(7):3849-56 Cancer Cell Int, 2013, 13(1):32	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.
S2012	PCI-34051 PCI-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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 BMC Biol, 2014, 12:95 Exp Mol Med, 2017, 49(2):e297	(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.
S1422	Droxinostat Droxinostat 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.	Nat Struct Mol Biol, 2013, 20(3):317-25 Clin Cancer Res, 2017, 23(12):3139-3149 Int J Cancer, 2016, 138(1):125-36	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).
S1090	Abexinostat (PCI-24781) Abexinostat (PCI-24781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with K_i of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.	Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130 Genet Mol Biol, 2014, 37(4):716-24	Differential effects of HDAC inhibitors on histone and tubulin acetylation. Immunofluorescence analysis of histone H3 (K9ac/K14ac) and tubulin acetylation in HeLa cells treated for 4 h with vehicle, SAHA (10 μM), tacedinaline (50 μM), PCI-24781 (20 μM. (a) Mapping of histone acetylation in K562 cells treated with HDAC inhibitors by LC-MS/MS. Cells were treated with TSA (10 μM), SAHA (5 μM), PCI-24781 (2 μM), tacedinaline (50 μM) for 6 h. Histones were extracted from cells and acetylated peptides were quantified after isobaric tagging.
S7229	RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.	Cell, 2019, 176(6):1447-1460 Leukemia, 2017, 31(12):2761-2770 J Invest Dermatol, 2017, 137(9):1935-1944	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.
S2244	AR-42 AR-42 is an HDAC inhibitor with IC50 of 30 nM. Phase 1.	Sci Transl Med, 2014, 6(256):256ra135 J Cell Physiol, 2018, 233(1):559-571 J Cell Physiol, 2019, 234(4):5252-5263	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.
S8001	Rocilinostat (ACY-1215) Ricolinostat (ACY-1215) 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. Phase 2.	Oncogene, 2017, 10.1038/onc.2016.495 J Pathol, 2018, 246(2):141-153 Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0481	(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.
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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
S2818	Tacedinaline (CI994) Tacedinaline (CI994) 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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Biol Chem, 2016, 291(14):7386-95 J Biomol Screen, 2011, 16(10):1247-53	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.
S2759	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. Phase 1.	J Cell Mol Med, 2018, 10.1111/jcmm.13935 Biochem Pharmacol, 2018, 148:13-26 Front Cell Infect Microbiol, 2018, 8:191	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.
S1999	Sodium butyrate Sodium butyrate, 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).	PLoS Biol, 2013, 12(1):e1001758 Br J Haematol, 2014, 167(5):639-50 Cancer Res, 2017, 77(18):5039-5053	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.
S1848	Curcumin Curcumin 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; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.	J Enzyme Inhib Med Chem, 2013, 10.3109/14756366.2013.837901 Nanotechnology, 2016, 27(35):355101 Eur J Pharmacol, 2017, 803:167-173	EC9706 and TE13 cells were treated with different concentrations of curcumin for 24 h. Then, cells were prepared for immunoblotting against p-JAK2, JAK2 and GAPDH.
S2779	M344 M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.	Biochem Biophys Res Commun, 2014, 445(2):320-6	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.
S2239	Tubacin Tubacin 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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 Leukemia, 2014, 28(3):680-9 PLoS Biol, 2013, 12(1):e1001758	Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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.	Neurochem Res, 2016, 41(12):3192-3205 The Winthrop McNair Research Bulletin, 2015, 1:17-22 Sci Rep, 2017, 7:43575	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.
S2693	Resminostat Resminostat 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.	Int J Oncol, 2018, 53(4):1469-1480 Head Neck, 2017, 39(5):900-907	Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
S1703	Divalproex Sodium Divalproex 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.	CNS Neurosci Ther, 2018, 24(5):404-411	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
S8043	Scriptaid Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.	J Antimicrob Chemother, 2014, 69(1):28-34 Hum Reprod, 2017, 32(1):76-87 Oncol Rep, 2018, 39(4):1999-2005	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).
S4125	Sodium Phenylbutyrate Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders.	Onco Targets Ther, 2016, 9:2825-33 CNS Neurosci Ther, 2018, 24(5):404-411 J Thromb Haemost, 2018, 16(10):2035-2043	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.
S8049	Tubastatin A Tubastatin 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).	Nat Commun, 2014, 5:3479 Leukemia, 2014, 28(3):680-9 Cell Rep, 2013, 5(6):1679-89	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.
S7324	TMP269 TMP269 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.	Clin Epigenetics, 2018, 10(1):100 J Biol Chem, 2016, 291(14):7386-95 J Cell Biochem, 2018, 119(4):3081-3090	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
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.	Neurochem Res, 2018, 43(6):1161-1170	Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
S8502	TMP195 TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
S3944	Valproic acid Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers.	J Trauma Acute Care Surg, 2017, 82(4):758-765
S7617	Tasquinimod Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.	Oxid Med Cell Longev, 2017, 7150376 J Mol Cell Biol, 2018, 10.1093/jmcb/mjy035 Oxid Med Cell Longev, 2017, 2017:7150376	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.
S7726	BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
S8464	Citarinostat (ACY-241) Citarinostat (ACY-241) 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.
S7593	Splitomicin Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.
S7278	HPOB HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.	Neurochem Int, 2016, 99:239-51 Molecules, 2018, 23(5)	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.
S7569	LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.	J Biol Chem, 2016, 291(14):7386-95 Clin Epigenetics, 2018, 10(1):120 Int J Mol Sci, 2018, 19(10)	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
S7473	Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.	Oncotarget, 2016, 7(39):63829-63838 Oncotarget, 2016, 7(23):34384-94	Cells were exposed to HDAC Class II selective inhibitors LMK-235 or Nexturastat A (NA) at the indicated concentrations for 48 hrs and analyzed by Western blotting. Rom, romidepsin; Bel, belinostat, Pano, panobinostat; SAHA, suberoylanilide hydroxamic acid.
S8567	Tucidinostat (Chidamide) Chidamide 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.
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.	J Neuroimmunol, 2017, 305:154-161 Harvard University, 2014, Kimberly Stegmaier Biochem Biophys Res Commun, 2018, 501(1):246-252	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
S8495	WT161 WT161 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.
S7596	CAY10603 CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.	Cancer Lett, 2016, 379(1):134-42 Med Oncol, 2016, 33(5):50 Oncol Rep, 2016, 36(1):589-97	U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
S8648	ACY-738 ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
S7555	4SC-202 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.
S7689	BG45 BG45 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.
S8323	ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.

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S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.	Nature, 2011, 471(7337):235-9 Nature, 2017, 551(7679):247-250 Nat Biotechnol, 2011, 29(3):255-65	Activity of vorinostat in Jurkat and Peer T-ALL cell lines in an MTT cell viability assay. Cells were treated with increasing drug concentrations for 72 h. The data are plotted as the mean % of DMSO-treated control cells against the corresponding drug concentration. The error bars are the standard error. For each drug and cell line, 3-4 independent experiments were performed with 6 replicates at each drug concentration.
S1053	Entinostat (MS-275) Entinostat (MS-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. Phase 3.	Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130 Nat Immunol, 2014, 15(5):439-48	(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.
S1030	Panobinostat (LBH589) Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.	Nat Biotechnol, 2011, 29(3):255-65 Nat Med, 2015, 10.1038/nm.3855 Cell, 2018, 173(6):1413-1425	(G) A375 parental and BRAFi-resistant ex vivo clones were treated with a panel of HDACi (1 μM vorinostat, 0.5 μM belinostat, and 6 nM panobinostat) in single treatment or in combination with 1 μM vemurafenib in a long-term colony formation assay.
S1045	Trichostatin A (TSA) Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.	Nature, 2017, 551(7679):247-250 Nat Biotechnol, 2015, 10.1038/nbt.3130 Cell, 2017, 171(4):824-835.e18	Gck expression in WT primary hepatocytes transduced with FOXO1 and KR-FOXO1 adenoviruses in the presence or absence of trichostatinA (TSA).
S1122	Mocetinostat (MGCD0103) Mocetinostat (MGCD0103) 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. Phase 2.	Nat Biotechnol, 2015, 10.1038/nbt.3130 Circ Res, 2012, 110(5):739-48 Blood, 2014, 123(10):1535-43	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.
S8773^新	TH34 TH34 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).
S5810^新	UF010 UF010 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.
S5905^新	Suberohydroxamic acid Suberohydroxamic acid is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively.
S9262^新	Raddeanin A Raddeanin A, a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity.
S5438^新	Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
S1085	Belinostat (PXD101) Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.	Nat Biotechnol, 2011, 29(3):255-65 Cell, 2018, 173(6):1413-1425 Clin Cancer Res, 2017, 23(12):3139-3149	A375DR and parental cells were seeded 50,000 cells per well in 6-well plates and treated with 1 mMvorinostat (Vor), 0.5 mMbelinostat (Bel), 5 nMpanobinostat (Pan), and/or combination of 5 nM trametinib and 0.125 mM dabrafenib.
S3020	Romidepsin (FK228, Depsipeptide) Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.	Nature, 2017, 551(7679):247-250 Blood, 2018, 131(4):397-407 Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384	Concentration over time for each dose cohort of romidepsin (B).
S1484	MC1568 MC1568 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.	Nat Commun, 2013, 4:2735 Proc Natl Acad Sci USA, 2012, 109(34):E2284-93 Diabetes, 2013, 63(2):645-54	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.
S2627	Tubastatin A HCl Tubastatin A HCl 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).	Int J Cancer, 2013, 134(11):2560-71 J Med Chem, 2015, 58(2):785-800 J Biol Chem, 2013, 288(20):14400-7	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.
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.	PLoS Pathog, 2014, 10(4):e1004071 Diabetologia, 2018, 61(2):389-398 J Neurosci, 2013, 33(17):7535-47	(e–h) Cytokine secretion. Pancreatic islets were isolated from 12-week (wk)-old non-diabetic, untreated diabetic or givinostat (Givi)-treated diabetic NOD-huCD3ε mice (after 3–4 weeks of treatment) (n = 5–9 per group). Islets were cultured at 37°C for 48 h and supernatant fractions were collected. Concentrations of (e) IL-1β, (f) IL-6, (g) TNF-α and (h) IL-10 were determined by ELISA; *p < 0.05.
S1095	Dacinostat (LAQ824) Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.	Nat Biotechnol, 2011, 29(3):255-65 Diabetologia, 2012, 55(9):2421-31 Cell Physiol Biochem, 2017, 41(3):1255-1266	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.
S1194	CUDC-101 CUDC-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.	J Chem Inf Model, 2014, 54(3):881-93 ACS Med Chem Lett, 2013, 4(9):858-62 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	(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.
S1096	Quisinostat (JNJ-26481585) 2HCl Quisinostat (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.	J Clin Oncol, 2016, 10.1200/JCO.2016.66.5547 Nat Commun, 2015, 6:8648 Nat Commun, 2013, 4:2735	In vitro drug sensitivity of (C) quisinostat. Acute lymphoblastic leukemia cell lines (NALM-6, KOPN-30bi) and primary cultured cells established from patient 21 were cultured with the indicated concentrations of anticancer drugs, and viability was measured at 48 hours. Data are presented as percentages of dimethylsulfoxide (DMSO) control and depict the mean 6 standard deviation.
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. Phase 2.	PLoS Pathog, 2014, 10(4):e1004071 Antimicrob Agents Chemother, 2012, 56(7):3849-56 Cancer Cell Int, 2013, 13(1):32	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.
S2012	PCI-34051 PCI-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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 BMC Biol, 2014, 12:95 Exp Mol Med, 2017, 49(2):e297	(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.
S1422	Droxinostat Droxinostat 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.	Nat Struct Mol Biol, 2013, 20(3):317-25 Clin Cancer Res, 2017, 23(12):3139-3149 Int J Cancer, 2016, 138(1):125-36	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).
S1090	Abexinostat (PCI-24781) Abexinostat (PCI-24781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with K_i of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.	Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130 Genet Mol Biol, 2014, 37(4):716-24	Differential effects of HDAC inhibitors on histone and tubulin acetylation. Immunofluorescence analysis of histone H3 (K9ac/K14ac) and tubulin acetylation in HeLa cells treated for 4 h with vehicle, SAHA (10 μM), tacedinaline (50 μM), PCI-24781 (20 μM. (a) Mapping of histone acetylation in K562 cells treated with HDAC inhibitors by LC-MS/MS. Cells were treated with TSA (10 μM), SAHA (5 μM), PCI-24781 (2 μM), tacedinaline (50 μM) for 6 h. Histones were extracted from cells and acetylated peptides were quantified after isobaric tagging.
S7229	RGFP966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.	Cell, 2019, 176(6):1447-1460 Leukemia, 2017, 31(12):2761-2770 J Invest Dermatol, 2017, 137(9):1935-1944	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.
S2244	AR-42 AR-42 is an HDAC inhibitor with IC50 of 30 nM. Phase 1.	Sci Transl Med, 2014, 6(256):256ra135 J Cell Physiol, 2018, 233(1):559-571 J Cell Physiol, 2019, 234(4):5252-5263	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.
S8001	Rocilinostat (ACY-1215) Ricolinostat (ACY-1215) 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. Phase 2.	Oncogene, 2017, 10.1038/onc.2016.495 J Pathol, 2018, 246(2):141-153 Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0481	(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.
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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
S2818	Tacedinaline (CI994) Tacedinaline (CI994) 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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Biol Chem, 2016, 291(14):7386-95 J Biomol Screen, 2011, 16(10):1247-53	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.
S2759	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. Phase 1.	J Cell Mol Med, 2018, 10.1111/jcmm.13935 Biochem Pharmacol, 2018, 148:13-26 Front Cell Infect Microbiol, 2018, 8:191	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.
S1999	Sodium butyrate Sodium butyrate, 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).	PLoS Biol, 2013, 12(1):e1001758 Br J Haematol, 2014, 167(5):639-50 Cancer Res, 2017, 77(18):5039-5053	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.
S1848	Curcumin Curcumin 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; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.	J Enzyme Inhib Med Chem, 2013, 10.3109/14756366.2013.837901 Nanotechnology, 2016, 27(35):355101 Eur J Pharmacol, 2017, 803:167-173	EC9706 and TE13 cells were treated with different concentrations of curcumin for 24 h. Then, cells were prepared for immunoblotting against p-JAK2, JAK2 and GAPDH.
S2779	M344 M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.	Biochem Biophys Res Commun, 2014, 445(2):320-6	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.
S2239	Tubacin Tubacin 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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 Leukemia, 2014, 28(3):680-9 PLoS Biol, 2013, 12(1):e1001758	Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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.	Neurochem Res, 2016, 41(12):3192-3205 The Winthrop McNair Research Bulletin, 2015, 1:17-22 Sci Rep, 2017, 7:43575	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.
S2693	Resminostat Resminostat 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.	Int J Oncol, 2018, 53(4):1469-1480 Head Neck, 2017, 39(5):900-907	Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
S1703	Divalproex Sodium Divalproex 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.	CNS Neurosci Ther, 2018, 24(5):404-411	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
S8043	Scriptaid Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.	J Antimicrob Chemother, 2014, 69(1):28-34 Hum Reprod, 2017, 32(1):76-87 Oncol Rep, 2018, 39(4):1999-2005	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).
S4125	Sodium Phenylbutyrate Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders.	Onco Targets Ther, 2016, 9:2825-33 CNS Neurosci Ther, 2018, 24(5):404-411 J Thromb Haemost, 2018, 16(10):2035-2043	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.
S8049	Tubastatin A Tubastatin 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).	Nat Commun, 2014, 5:3479 Leukemia, 2014, 28(3):680-9 Cell Rep, 2013, 5(6):1679-89	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.
S7324	TMP269 TMP269 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.	Clin Epigenetics, 2018, 10(1):100 J Biol Chem, 2016, 291(14):7386-95 J Cell Biochem, 2018, 119(4):3081-3090	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
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.	Neurochem Res, 2018, 43(6):1161-1170	Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
S8502	TMP195 TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
S3944	Valproic acid Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers.	J Trauma Acute Care Surg, 2017, 82(4):758-765
S7617	Tasquinimod Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.	Oxid Med Cell Longev, 2017, 7150376 J Mol Cell Biol, 2018, 10.1093/jmcb/mjy035 Oxid Med Cell Longev, 2017, 2017:7150376	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.
S7726	BRD73954 BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
S8464	Citarinostat (ACY-241) Citarinostat (ACY-241) 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.
S7593	Splitomicin Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.
S7278	HPOB HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.	Neurochem Int, 2016, 99:239-51 Molecules, 2018, 23(5)	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.
S7569	LMK-235 LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.	J Biol Chem, 2016, 291(14):7386-95 Clin Epigenetics, 2018, 10(1):120 Int J Mol Sci, 2018, 19(10)	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
S7473	Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.	Oncotarget, 2016, 7(39):63829-63838 Oncotarget, 2016, 7(23):34384-94	Cells were exposed to HDAC Class II selective inhibitors LMK-235 or Nexturastat A (NA) at the indicated concentrations for 48 hrs and analyzed by Western blotting. Rom, romidepsin; Bel, belinostat, Pano, panobinostat; SAHA, suberoylanilide hydroxamic acid.
S8567	Tucidinostat (Chidamide) Chidamide 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.
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.	J Neuroimmunol, 2017, 305:154-161 Harvard University, 2014, Kimberly Stegmaier Biochem Biophys Res Commun, 2018, 501(1):246-252	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
S8495	WT161 WT161 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.
S7596	CAY10603 CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.	Cancer Lett, 2016, 379(1):134-42 Med Oncol, 2016, 33(5):50 Oncol Rep, 2016, 36(1):589-97	U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
S8648	ACY-738 ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
S7555	4SC-202 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.
S7689	BG45 BG45 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.