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ALK5 protein kinase inhibitor IN 1130, 5 mg  

ALK5 protein kinase inhibitor IN 1130, 5 mg

3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide

IN 1130 is a highly selective small molecule ALK5 inhibitor

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PKI-IN1130-005

Availability: within 3 days

187,50 €

Background: IN 1130 is a highly selective small molecule ALK5 inhibitor (IC50 value of 5.3 nM for inhibition of ALK5-mediated Smad3 phosphorylation) with >100 fold selectivity over p38α and a panel of 26 other serine/threonine and tyrosine kinases. Suppressor of fibrogenic process of unilateral ureteral obstruction in rats underscoring the potential clinical benefits in the treatment of renal fibrosis. By inhibition of TGF-β signaling, IN1130 ameliorated experimental autoimmune encephalomyelitis, lessened tunical fibrosis and corrected penile curvature in rats, inhibited cancer metastasis in MMTV/c-Neu breast cancer mice, and enhanced CTL response in cancer mice.

Chemical formula: C25H20N6O
Molecular weight: 420.47 g/mol
Purity: 99 %
Appearance: Yellow solid
Solubility: Soluble in DMSO
CAS Number: 868612-83-3

Manufacturer:  Axon Medchem BV

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

References

C.Y. Park et al. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80.
 
C.H. Jin et al. Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. Bioorg Med Chem. 2011 Apr 15;19(8):2633-40.
 
J.A. Moon et al. IN-1130, a novel transforming growth factor-bold italic beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney International (2006) 70, 1234–1243.
 
G.T. Lee et al. Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/activin receptor-like kinase-5, on prostate cancer cells. J Urol. 2008 Dec;180(6):2660-7.
 
J.K. Ryu et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (activin receptor-like kinase 5) inhibitor, promotes regression of fibrotic plaque and corrects penile curvature.... J Sex Med. 2009 May;6(5):1284-96.

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