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ALK protein kinase inhibitor SB 431542, 5 mg  

ALK protein kinase inhibitor SB 431542, 5 mg

4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide

Synonyms: SB-431542, SB431542
ATP competitive inhibitor of TGF-β superfamily members ALK5, ALK4 and ALK7

More details

PKI-SB431-005

Availability: within 7 days

110,50 €

Background: SB-431542 acts as an ATP competitive inhibitor of TGF-β superfamily members ALK5, ALK4 (IC50 of 94 nM, 140 nM) and ALK7 and has less inhibitory potency on a panel of other kinases tested (weak inhibitory activity on p38α with an IC50 of 10 µM). It inhibits TGF-β- and activin-induced phosphorylation of Smad2/Smad4 and Smad3/Smad4 dependent transcription, which is mediated by ALK5 and ALK4, respectively, but not BMP-induced phosphorylation of Smad1, which is mediated by ALKs 2, 3, and 6.

Formula: C22H16N4O3
Chemical Name: 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2- yl]benzamide
Molecular Weight: 384.39 g/mol
Purity:  >99%
Appearance:  White solid
Solubility:  in DMSO to 100 mM
CAS No.:  301836-41-9
Manufacturer: Axon Medchem

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.

Product specific literature references:

Inman GJ, Nicolas FJ, Callahan JF, Harling JD, Gaster LM, Reith AD, Laping NJ, Hill CS. (2002) SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol 62(1) 65-74

Callahan JF, Burgess JL, Fornwald JA, Gaster LM, Harling JD, Harrington FP, Heer J, Kwon C, Lehr R, Mathur A, Olson BA, Weinstock J, Laping NJ.(2002) “Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).” J Med Chem. 28;45(5):999-1001.

Harrison CA, Gray PC, Vale WW, Robertson DM.(2005)“ Antagonists of activin signaling: mechanisms and potential biological applications.” Trends Endocrinol Metab. 2005 Mar;16(2):73-8

Tanaka H, Shinto O, Yashiro M, Yamazoe S, Iwauchi T, Muguruma K, Kubo N, Ohira M, Hirakawa K. (2010) “Transforming growth factor β signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity.” Oncol Rep.;24(6):1637-43.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.