616461

TGF-β RI Kinase Inhibitor VI, SB431542

TGF-β RI Kinase Inhibitor VI, SB431542, CAS 301836-41-9, is a cell-permeable inhibitor of SMAD2 phosphorylation. Inhibits the activity of ALK4 and ALK5 (IC₅₀ = 140 nM and 94 nM, respectively).

• Synonym(s): TGF-β RI Kinase Inhibitor VI, SB431542, 4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, SB-431542
• CAS Number: 301836-41-9
• MDL number: MFCD27976360
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Quality Level: 300
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: ethanol: 10 mg/mL; DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [nH]1c(nc(c1c4cc5c(cc4)OCO5)c3ncccc3)c2ccc(cc2)C(=O)N
• 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)
• InChI key: FHYUGAJXYORMHI-UHFFFAOYSA-N

Description

General description

A cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 µM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC₅₀ = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC₅₀ ≥10 µM in the presence of 10 µM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable