301836-41-9 Usage
Description
SB 431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5, belonging to the class of benzamides. It is a cell-permeable triarylimidazole compound that effectively inhibits cellular Smad2 phosphorylation and blocks transforming growth factor-β1-induced cell migration and invasion in carcinoma cells. SB 431542 specifically targets ALK4 and ALK5, with little to no effect on other kinases, making it a potent TGF-beta inhibitor.
Uses
Used in Pharmaceutical Industry:
SB 431542 is used as a Src family kinase inhibitor for blocking TGF-β1-induced cell migration and invasion in both established and primary carcinoma cells. This application is particularly relevant in the development of treatments for various types of cancer.
Used in Research Applications:
SB 431542 is used as a research tool for studying the role of TGF-β1 signaling in cell migration, invasion, and fibrosis. It is also used to investigate the effects of ALK/Smad signaling on stem cell renewal and differentiation.
Used in Drug Development:
SB 431542 is used in the development of novel drug delivery systems to enhance its applications and efficacy against cancer cells. It is employed in combination with other compounds, such as PD0325901 and Thiazovivin, to improve the efficiency of human iPSCs generation from fibroblast cultures.
Biological Activity
Potent and selective inhibitor of the transforming growth factor- β (TGF- β ) type I receptor activin receptor-like kinase ALK5 (IC 50 = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF- β -induced proliferation of human osteosarcoma cells. Stimulates proliferation, differentiation and sheet formation of ESC-derived endothelial cells.
Biochem/physiol Actions
SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.
References
1) Laping et al. (2002), Inhibition of transforming growth factor (TGF-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I kinase activity: SB-431542; Mol. Pharmacol., 62 58
2) Inman et al. (2002), 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; Mol. Pharmacol., 62 65
3) Matsuyama et al. (2003), SB-431542 and Gleevec inhibit transforming growth factor-beta-induced proliferation of human osteosarcoma cells; Cancer Res., 63 7791
4) Watabe et al. (2003), TGF-beta receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells; J. Cell Biol., 163 1303
5) Stanslowsky et al. (2014), Functional differentiation of midbrain neurons from human cord blood-derived induced pluripotent stem cells; Stem Cell Res. Ther., 5 35
Check Digit Verification of cas no
The CAS Registry Mumber 301836-41-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,0,1,8,3 and 6 respectively; the second part has 2 digits, 4 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 301836-41:
(8*3)+(7*0)+(6*1)+(5*8)+(4*3)+(3*6)+(2*4)+(1*1)=109
109 % 10 = 9
So 301836-41-9 is a valid CAS Registry Number.
InChI:InChI=1/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)
