616464

SB431542

≥97% (HPLC), liquid, TGF-β RI kinase inhibitor, Calbiochem^®

• Synonym(s): InSolution TGF-β RI Kinase Inhibitor VI, SB431542
• Empirical Formula (Hill Notation): C₂₂H₁₆N₄O₃ · 2H₂O
• CAS Number: 301836-41-9
• Molecular Weight: 420.42
• MDL number: MFCD27976360
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Product Name: TGF-β RI Kinase Inhibitor VI, SB431542, InSolution, ≥97%
• Quality Level: 100
• assay: ≥97% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• shipped in: ambient
• storage temp.: −20°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: Irritant (B)

Physical form

A 100 mM (5 mg/119 µl) solution of SB431542 (Cat. No. 616461) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Other Notes

Ikushima, H., et al. 2009. Cell Stem Cell5, 504.
Lin, T., et al. 2009. Nat. Methods6, 805.
Maherali, N. and Hochedlinger, K., 2009. Curr. Biol.19, 1718.
Callahan, J.F., et al. 2002. J. Med. Chem.45, 999.
Inman, G.J., et al. 2002. Mol. Pharmacol.62, 65.
Laping, N.J., et al. 2002. Mol. Pharmacol.62, 58.

Legal Information

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

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk_germany: WGK 1
• flash_point_f: 188.6 °F - (refers to pure substance)
• flash_point_c: 87 °C - (refers to pure substance)