Molecular Weight(MW): 384.39
SB431542 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.
Cited by 24 Publications
9 Customer Reviews
Hedgehog, Igf and Tgf signaling are required for myocardial regeneration in zebrafish. (C) Quantification of the effects of CyA (10 uM), NVP AEW541 (2 uM) and SB-431542 (10 uM) on cardiomyocyte proliferation after resection injury. Fish were treated from 6 to 7 dpa. (D) Quantification of the effects of CyA, NVP AEW541 and SB-431542 on proliferation after genetic cardiomyocyte ablation.
Development 2013 140, 660-666. SB431542 purchased from Selleck.
Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01.
Acta Biomater 2014 10(7):3108-16. SB431542 purchased from Selleck.
Transforming growth factor-b (TGF-b)/Smad3 induces Akt phosphorylation in vascular smooth muscle cells (SMCs). C: vascular SMCs were pretreated with the TGF- receptor inhibitor SB431542 (10 uM) for 30 min and then stimulated with TGF- (5 ng/ml) for 12 h, and p-Akt was measured by Western blot analysis.
Am J Physiol Heart Circ Physiol 2012 302, H2211-H2219. SB431542 purchased from Selleck.
Effect of small molecule inhibitors on reprogramming efficiency of myoblast cell derived from 5 different donors. (A) Reprogramming efficiency is shown as number of colonies from 10^5 starting cells on Y-axes. Ctrl, control condition and addition of small molecule inhibitors are marked. (B) AP staining of reprogrammed myoblast cell lines, from 5 different donors, in wells of 12-well plates at day 18. Ctrl, control condition and additions of small molecule inhibitors are marked.
Stem Cells Dev 2013 SB431542 purchased from Selleck.
Retroviral reprogramming of myoblasts. (C) Small molecule inhibitors effect on reprogramming efficiency compared to control. (D) AP staining of reprogrammed plates with or without inhibitors. Close-up of AP staining, bar 500 um; AP, alkaline phosphatase.
Stem Cells Dev 2013 SB431542 purchased from Selleck.
TGFb1 mRNA expression in different follicles of the 26 weeks old hen ovaries and its effect on CTGF mRNA expression in granulosa cells. Effects of TGFb1 and inhibitor SB431542 on CTGF mRNA expression in granulosa cells from F2 to F4 and POF1 follicles.
Gen Comp Endocr 2012 178, 314–322. SB431542 purchased from Selleck.
SB431542 inhibit expression of TGF-beta induced pS2 in MvILu cell
Dr. Kah-Wai Lin of Karolinska Biomics Center. SB431542 purchased from Selleck.
(C) C3H10T1/2 cells transfected with pEF-BOS or pEF-Flag-TAZ were cultured for 8 days in osteogenic medium (OM) including ascorbic acid and β-glycerophosphate in the absence or presence of TGF-β inhibitors (SB-431542 or SB-525334). ALP activity was measured in the cell layer and normalized to cellular protein content. Data are expressed as means 6 ± SD ( *p < 0.05 vs. pEF-BOS, # p < 0.01 vs. vehicle) (D) Quantitative RT-PCR analysis of Col 1 and ALP in C3H10T1/2 cells.
SB431542 purchased from Selleck.
Purity & Quality Control
Choose Selective TGF-beta/Smad Inhibitors
|Description||SB431542 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.|
SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription.  In A498 cells, SB 431542 inhibits both TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 of 60 nM and 50 nM, respectively. In addition, SB 431542 inhibits production of TGF-β1-induced fibronectin mRNA and protein with IC50 of 62 nM and 22 nM, respectively.  SB 431542 blocks the TGF-β-mediated growth factors, including PDGF-A, FGF-2 and HB-EGF, leading to an increase in proliferation of MG63 cells. SB 431542 also inhibits TGF-β-induced c-Myc and p21 WAF1/CIP1.  SB 431542 significantly suppresses TGF-β-induced G1 arrest, leading to accumulation of cells in the S phase of the cell cycle in FET, RIE, and Mv1Lu cells. SB 431542 also inhibits TGF-β-induced epithelial to mesenchymal transition (EMT) in NMuMG and PANC-1 cells.  SB 431542 significantly elevates the expression of CD86 in BM-DCs and that of CD83 within CD11c+ cells suppressed by TGF-β. SB 431542 is able to induce NK activity through functional maturation and IL-12 production of human DCs. 
|In vivo||SB 431542 triggers cytotoxic T lymphocyte (CTL) activities in the colon-26 carcinoma models and is most likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGF-β. |
|Kinase Assay: ||
Flashplate assay for ALK5:SB 431542 is dissolved in DMSO at a concentration of 10 mM. The kinase domain of TGFβRI, from amino acid 200 to the C-terminus, and the full-length Smad3 protein are expressed as N-terminal glutathion S-transferase (GST) fusion proteins in the baculovirus expression system. Proteins are purified with glutathion Sepharose beads 4B. Basic FlashPlates are coated with 0.1 M sterile filtered sodium bicarbonate, pH 7.6, containing 700 ng of GST-Smad3 per 100 μL. Assay buffer contains 50 mM HEPES (pH 7.4), 5 mM MgCl2, 1 mM CaCl2, 1 mM DTT, 100 mM GTP, 3 μM ATP plus 0.5 μCi/well ɤ33P-ATP, and 85 ng of GST-ALK5 with or without SB 431542. Plates are incubated at 30 °C for 3 hours. The assay buffer is removed by aspiration, and the plate is counted on a Packard TopCount 96-well scintillation plate reader.
-  Callahan JF, et al. J Med Chem, 2002, 45(5), 999-1001.
-  Inman GJ, et al. Mol Pharmacol, 2002, 62(1), 65-74.
-  Laping NJ, et al. Mol Pharmacol, 2002, 62(1), 58-64.
|In vitro||DMSO||76 mg/mL (197.71 mM)|
|Ethanol||3 mg/mL (7.8 mM)|
|In vivo||Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
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Frequently Asked Questions
I would appreciate it if you can help me in figuring out the formulation for this drug in vivo experiments.
S1067 SB431542 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension for oral gavage. It can also be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml as a clear solution for IP injection.