产品名称

IN 1130

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Axon 2236 CAS [868612-83-3] MF C25H20N6OMW 420.47 Purity: 99% Soluble in DMSO Description 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. References Certificates Categories Extra info 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. Certificate of Analysis Material Safety Data Sheet Apoptosis Cell Signaling & Oncology Stem Cell TGF-β RSTK class I; EC 2.7.11.30 TGF-βR TGF-βR 1 inhibitor Chemical name 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide Parent CAS No. [868612-83-3] Order Size Unit Price Stock 5 mg €105.00 In Stock

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现货询价，电话：010-67529703

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axonmedchem

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IN 1130

Based on 16 reference(s) in Google Scholar 9 10 16

Axon 2236

CAS [868612-83-3]

MF C25H20N6O
MW 420.47

Purity: 99%
Soluble in DMSO

IN 1130

Description

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.