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SB-431542

SB-431542

  • CAT Number: I003052
  • CAS Number: 301836-41-9
  • Molecular Formula: C22H16N4O3
  • Molecular Weight: 384.39
  • Purity: ≥95%
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SB-431542 (CAT: I003052) is a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptor, also known as the activin receptor-like kinase (ALK) 5. It is widely used in biological and pharmaceutical research to study the TGF-β signaling pathway and its role in various cellular processes. SB-431542 specifically blocks the kinase activity of ALK5, preventing the phosphorylation of downstream signaling molecules and inhibiting TGF-β signaling. This compound has been employed to investigate the involvement of TGF-β signaling in processes such as cell differentiation, development, fibrosis, and cancer progression. SB-431542’s targeted inhibition of ALK5 makes it a valuable tool for understanding TGF-β signaling and exploring potential therapeutic applications.

Catalog Number I003052
CAS Number 301836-41-9
Molecular Formula

C22H16N4O3

Purity 95%
Target TGF-βR1(ALK5)
Solubility DMSO: ≥ 40 mg/mL
Storage 3 years -20C powder
Overview of Clinical Research

<span style=”color:#000000;”><span style=”font-family:arial,helvetica,sans-serif;”><span style=”font-size:12px;”>SB431542 is a&nbsp;<span style=”font-variant-ligatures: normal; orphans: 2; widows: 2;”>Transforming growth factor beta1 inhibitor. The p</span><span style=”font-variant-ligatures: normal; orphans: 2; widows: 2;”>reclinical trials in Wounds in USA (unspecified route) are ongoing.</span></span></span></span>

IC50 94 nM (ALK5)[1], 94 nM (Smad3)[2]
IUPAC Name 4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide
InChI InChI=1S/C22H16N4O3/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17/h1-11H,12H2,(H2,23,27)(H,25,26)
InChIKey FHYUGAJXYORMHI-UHFFFAOYSA-N
SMILES C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5
Reference

<br />
1:SB-431542, a specific inhibitor of the TGF-&beta; type I receptor inhibits hypoxia-induced proliferation of pulmonary artery adventitial fibroblasts. Yuan W, Liu W, Cai H, Sun X, Yang D, Xu F, Jin C.Pharmazie. 2016 Feb;71(2):94-100. PMID: 27004374<br />
2:Transforming growth factor &beta; signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Tanaka H, Shinto O, Yashiro M, Yamazoe S, Iwauchi T, Muguruma K, Kubo N, Ohira M, Hirakawa K.Oncol Rep. 2010 Dec;24(6):1637-43. PMID: 21042762<br />
3:Enhanced differentiation of human embryonic stem cells to mesenchymal progenitors by inhibition of TGF-beta/activin/nodal signaling using SB-431542. Mahmood A, Harkness L, Schr&oslash;der HD, Abdallah BM, Kassem M.J Bone Miner Res. 2010 Jun;25(6):1216-33. doi: 10.1002/jbmr.34. PMID: 20200949 Free Article<br />
4:SB-431542 inhibition of scar formation after filtration surgery and its potential mechanism. Xiao YQ, Liu K, Shen JF, Xu GT, Ye W.Invest Ophthalmol Vis Sci. 2009 Apr;50(4):1698-706. doi: 10.1167/iovs.08-1675. Epub 2008 Dec 20. PMID: 19098325<br />
5:SB-431542, a transforming growth factor beta inhibitor, impairs Trypanosoma cruzi infection in cardiomyocytes and parasite cycle completion. Waghabi MC, Keramidas M, Calvet CM, Meuser M, de Nazar&eacute; C Soeiro M, Mendon&ccedil;a-Lima L, Ara&uacute;jo-Jorge TC, Feige JJ, Bailly S.Antimicrob Agents Chemother. 2007 Aug;51(8):2905-10. Epub 2007 May 25. PMID: 17526757 Free PMC Article<br />
6:SB-431542 inhibits TGF-beta-induced contraction of collagen gel by normal and keloid fibroblasts. Hasegawa T, Nakao A, Sumiyoshi K, Tsuchihashi H, Ogawa H.J Dermatol Sci. 2005 Jul;39(1):33-8. PMID: 15978417<br />
7:A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Halder SK, Beauchamp RD, Datta PK.Neoplasia. 2005 May;7(5):509-21. PMID: 15967103 Free PMC Article<br />
8:SB-431542, a small molecule transforming growth factor-beta-receptor antagonist, inhibits human glioma cell line proliferation and motility. Hjelmeland MD, Hjelmeland AB, Sathornsumetee S, Reese ED, Herbstreith MH, Laping NJ, Friedman HS, Bigner DD, Wang XF, Rich JN.Mol Cancer Ther. 2004 Jun;3(6):737-45. PMID: 15210860 Free Article<br />
9:SB-431542 and Gleevec inhibit transforming growth factor-beta-induced proliferation of human osteosarcoma cells. Matsuyama S, Iwadate M, Kondo M, Saitoh M, Hanyu A, Shimizu K, Aburatani H, Mishima HK, Imamura T, Miyazono K, Miyazawa K.Cancer Res. 2003 Nov 15;63(22):7791-8. PMID: 14633705 Free Article<br />
10:SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Inman GJ, Nicol&aacute;s FJ, Callahan JF, Harling JD, Gaster LM, Reith AD, Laping NJ, Hill CS.Mol Pharmacol. 2002 Jul;62(1):65-74. PMID: 12065756 Free Article

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