SB-431542 is a novel small molecule inhibitor of the type I TGF-beta receptor, on a panel of human malignant glioma cell lines. SB-431542 blocked the phosphorylation and nuclear translocation of the SMADs, intracellular mediators of TGF-beta signaling, with decreased TGF-beta-mediated transcription. Furthermore, SB-431542 inhibited the expression of two critical effectors of TGF-beta-vascular endothelial growth factor and plasminogen activator inhibitor-1.
Chemical Formula: C22H16N4O3
Exact Mass: 384.12224
Molecular Weight: 384.39
Elemental Analysis: C, 68.74; H, 4.20; N, 14.58; O, 12.49
Chemical Name: 4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide
InChi Code: 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)
Appearance: white to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC50 values of 62 and 22 nM, respectively. SB-431542 (10 μM) is a selective inhibitor of TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells.
SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft.
- Tanaka H, Shinto O, Yashiro M, Yamazoe S, Iwauchi T, Muguruma K, Kubo N, Ohira M, Hirakawa K. Transforming growth factor β signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Oncol Rep. 2010 Dec;24(6):1637-43. PubMed PMID: 21042762.
- Mahmood A, Harkness L, SchrÃ¸der HD, Abdallah BM, Kassem M. Enhanced differentiation of human embryonic stem cells to mesenchymal progenitors by inhibition of TGF-beta/activin/nodal signaling using SB-431542. J Bone Miner Res. 2010 Jun;25(6):1216-33. PubMed PMID: 20200949.
- Xiao YQ, Liu K, Shen JF, Xu GT, Ye W. SB-431542 inhibition of scar formation after filtration surgery and its potential mechanism. Invest Ophthalmol Vis Sci. 2009 Apr;50(4):1698-706. Epub 2008 Dec 20. PubMed PMID: 19098325.
- Waghabi MC, Keramidas M, Calvet CM, Meuser M, de NazarÃ© C Soeiro M, MendonÃa-Lima L, AraÃºjo-Jorge TC, Feige JJ, Bailly S. SB-431542, a transforming growth factor beta inhibitor, impairs Trypanosoma cruzi infection in cardiomyocytes and parasite cycle completion. Antimicrob Agents Chemother. 2007 Aug;51(8):2905-10. Epub 2007 May 25. PubMed PMID: 17526757; PubMed Central PMCID: PMC1932517.
- Hasegawa T, Nakao A, Sumiyoshi K, Tsuchihashi H, Ogawa H. SB-431542 inhibits TGF-beta-induced contraction of collagen gel by normal and keloid fibroblasts. J Dermatol Sci. 2005 Jul;39(1):33-8. PubMed PMID: 15978417.
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