TGF-beta/Smad
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1067 | SB431542 | <1 mg/mL | 76 mg/mL | 3 mg/mL |
| S2618 | LDN-193189 | <1 mg/mL | <1 mg/mL | <1 mg/mL |
| S2230 | Galunisertib (LY2157299) | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2704 | LY2109761 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S1476 | SB525334 | <1 mg/mL | 68 mg/mL | 68 mg/mL |
| S2186 | SB505124 | <1 mg/mL | 67 mg/mL | 67 mg/mL |
| S2907 | Pirfenidone | <1 mg/mL | 37 mg/mL | 37 mg/mL |
| S2750 | GW788388 | <1 mg/mL | 15 mg/mL | <1 mg/mL |
| S2805 | LY364947 | <1 mg/mL | 1 mg/mL | <1 mg/mL |
| S7223 | RepSox | <1 mg/mL | 57 mg/mL | <1 mg/mL |
| S7507 | LDN-193189 HCl | 52 mg/mL | <1 mg/mL | <1 mg/mL |
| S7359 | K02288 | <1 mg/mL | 70 mg/mL | <1 mg/mL |
| S7624 | SD-208 | <1 mg/mL | 9 mg/mL | <1 mg/mL |
| S7627 | LDN-214117 | <1 mg/mL | 83 mg/mL | 83 mg/mL |
| S7959 | SIS3 HCl | <1 mg/mL | 97 mg/mL | 24 mg/mL |
| S7530 | Vactosertib (TEW-7197) | <1 mg/mL | 79 mg/mL | 43 mg/mL |
| S7146 | DMH1 | <1 mg/mL | 22 mg/mL | <1 mg/mL |
| S7147 | LDN-212854 | <1 mg/mL | 81 mg/mL | <1 mg/mL |
| S7148 | ML347 | <1 mg/mL | 10 mg/mL | <1 mg/mL |
| S7658 | Kartogenin | <1 mg/mL | 63 mg/mL | 5 mg/mL |
| S2308 | Hesperetin | <1 mg/mL | 60 mg/mL | <1 mg/mL |
| S8318 | Alantolactone | <1 mg/mL | 46 mg/mL | 46 mg/mL |
- TGF-beta/Smad阻害剤(22)
| 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 |
|---|---|---|---|
| S1067 |
SB431542SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases. |
Phase-contrast images of RPBJ- and HNF6-deficient hepatocyte spheroids embedded in collagen gels and cultured in the presence or absence of the TGFβ inhibitor SB-431542 (SB) for the indicated number of days.
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| S2618 |
LDN-193189LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. |
LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment. |
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| S2230 |
Galunisertib (LY2157299)Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3. |
Treatment of HLE and HLF cells with TGFβRI inhibitor LY2157299 led to dose-dependent loss of GLI2 levels.
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| S2704 |
LY2109761LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. |
C, Western blot analysis of serum cultured GB2 cells treated with each 20 μm inhibitor. The representative Western blot is shown for each protein and the bar charts represent the quantified values (mean ± s.d.) of three replicates. The fold changes were normalized by the relative densities regarding α-Tubulin.
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| S1476 |
SB525334SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. |
Immunoprecipitation and immunoblotting of wild-type cells treated as indicated (n = 3 experiments). i=TGFβR inhibitor:SB525334.
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| S2186 |
SB505124SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6. |
(D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.
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| S2907 |
PirfenidonePirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3. |
(E, F) Western Blot analysis of phLF isolated from (E) IPF patients or (F) donors treated for 48h with increasing concentrations of nintedanib (0.01, 0.1, 1 μM) or pirfenidone (100, 500, 1000 μM) in absence or presence of TGF-β1 (2 ng/mL). Densitometric analysis and representative blots show the effect of nintedanib and pirfenidone on collagen I (Col I) protein expression relative to β-actin as loading control (ACTB). Data are based on 8 (IPF) or 3 (donor) completely independent experiments and are given as mean ± SEM. Statistical significance between control and different concentrations of nintedanib or pirfenidone is indicated by horizontal brackets and asterisks. |
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| S2750 |
GW788388GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor. |
Combination treatment with GW788388 and IL-23 aiming to sustain Th17 cell levels increases spleen cell production of the inflammatory mediators IL-17 and TNF-a, the stimulatory mediators IL-2, IFN-g and RANTES, and the inhibitory mediator IL-10. Starting from Week 6 of 4NQO administration, when premalignant oral lesions were detectable on the tongue, mice were initiated on treatment with diluent, GW788388, IL-23 or both GW788388 and IL-23. After 2 months of these treatments, spleens were collected and cultured on anti-CD3 for 3 days. Supernatants were collected and used for measurement of the inflammatory mediators IL-17, TNF-a and IL-6 (a); stimulatory mediators IL-2, IFN-g and RANTES (b); and inhibitory mediators, TGF-b, IL-4 and IL-10 (c). *=p<0.05, **=p<0.01, ***=p<0.001.
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| S2805 |
LY364947LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II. |
The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively. |
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| S7223 |
RepSoxRepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively. |
(C) Generation of pluripotent stem cell from Yamanaka factors-induced OG2-MEFs under treatment of diverse chemical compounds. Images of GFP+ colonies were taken on day 10 post-infection. VPA, 0.5 mmol/L. CHIR99021, 3 μmol/L. Repsox, 1 μmol/L. (D) Quantification of GFP+ colonies in (C). All figures are representative of three independent experiments (n = 3). All data are presented as mean ± SD. *P < 0.05, **P < 0.01 vs. DMSO
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| S7507 |
LDN-193189 HClLDN193189 HCl is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β. |
LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
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| S7359 |
K02288K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA. |
A549 cells were transfected with miR-205 inhibitor (IHT-205, 100 nM). Forty hours after transfection, the cells were seeded on transwell plates and treated with or without inhibitor K02288 (10 nM), AG1478 (1 µM), SB431542 (10 µM) for 10 hours. Migrated cells were quantified. All data are shown as mean± SD. N =3. All experiments have been repeated at least 3times independently. |
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| S7624 |
SD-208SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. |
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| S7627 |
LDN-214117LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM. |
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| S7959 |
SIS3 HClSIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways. |
Cultured cardiac fibroblasts infected with vector lentiviruses or EphrinB2 overexpressing lentiviruses were stimulated with specific antagonist against Stat3 (Stattic, 2.5μM) and/or Smad3 (SIS3, 1μM), respectively. The expression level of α-SMA was quantified via western blotting. In vitro experiments repeat 3 times, *P<0.05, **P<0.01. |
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| S7530 |
Vactosertib (TEW-7197)Vactosertib (TEW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1. |
Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.
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| S7146 |
DMH1DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. |
The combined treatment with miR-140-5p mimics and some common chemotherapeutics did not have any effect on the SK-MES1 cell line, whereas miR-140-5p and DMH1 and cisplatin decreased the proliferation of
the A549 cells. Data are presented as mean±SEM of three individual experiments undertaken in triplicate. t-Test was used to assess significance with *p<0.05.
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| S7147 |
LDN-212854LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively. |
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| S7148 |
ML347ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM. |
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| S7658 |
KartogeninKartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes. |
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| S2308 |
HesperetinHesperetin is a bioflavonoid and, to be more specific, a flavanone. |
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| S8318 |
AlantolactoneAlantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction. |
Colon cancer cell lines (A) SW620, (B) HCT116, and (C) HT29 were treated with different concentrations (60, 12, 2.4, 0.48, and 0.098 μM) of nifuroxazide (nifu), niclosamide (nicl), cryptotanshinone (cry), and a lantolactone (ala), respectively, for 72 h. Cell proliferation in each group was detected by MTT assay. (D) HCT116, SW620, and HT29 cell lines were suppressed with niclosamide treatment at different concentrations (20, 10, 5, 2.5, and 1.25 μM) for 72 h. Subsequently, cell proliferation in each group was detected by MTT assay. The data were obtained from 3 independent experiments.
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