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IN 1130
- Soluble in DMSO
- MF: C25H20N6O
- MW: 420.47
Description
IN 1130 is a highly selective ALK5/TGF-β receptor type 1 inhibitor with reported IC50 of 5.3 nM for inhibition of ALK5-mediated SMAD3 phosphorylation. It shows more than 100-fold selectivity over p38α and a panel of other serine/threonine and tyrosine kinases.
TGF-β/ALK5 signaling drives fibrosis, immune regulation, tumor progression and tissue remodeling. IN 1130 is relevant for studying SMAD3-dependent TGF-β signaling in renal fibrosis, autoimmune encephalomyelitis, tunical fibrosis and cancer metastasis models.
Key Features
- Highly selective ALK5 inhibitor
- Blocks ALK5-mediated SMAD3 phosphorylation
- Selectivity over p38α and broad kinase panels reported
- Active in fibrosis, autoimmune and cancer models
Applications
- TGF-βR1/ALK5 signaling studies
- SMAD3 phosphorylation assays
- Fibrosis model research
- Cancer metastasis and immune-response studies
More Information
| Parent CAS No. | 868612-83-3 |
|---|---|
| Chemical Name | 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide |
| SMILES | C(N)(=O)C1=CC=CC(CC2NC(C3=NC(C)=CC=C3)=C(C3=CC=C4C(=C3)N=CC=N4)N=2)=C1 |
| MFCD | MFCD19441274 |
| InChi | InChI=1S/C25H20N6O/c1-15-4-2-7-20(29-15)24-23(17-8-9-19-21(14-17)28-11-10-27-19)30-22(31-24)13-16-5-3-6-18(12-16)25(26)32/h2-12,14H,13H2,1H3,(H2,26,32)(H,30,31) |
| InChiKey | RYKSGWSKILPDDY-UHFFFAOYSA-N |
| CID | 11676119 |
| Short Description | ALK5 inhibitor |
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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