868612-83-3
Chemical Structure
IN-1130
- CAS No.: 868612-83-3
- Formula:C25H20N6O
- Molecular Weight:420.47
IUPAC Name: 3-((4-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide
InChIKey: RYKSGWSKILPDDY-UHFFFAOYSA-N
SMILES: O=C(N)C1=CC=CC(CC2=NC(C3=NC(C)=CC=C3)=C(C4=CC=C5N=CC=NC5=C4)N2)=C1
Biological Activity: IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis[1][2].
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IN-1130 | 99.93% | IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis. | ||||||||||||||||||||
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IN-1130 (Standard) | ≥98% | IN-1130 (Standard) is the analytical standard of IN-1130. This product is intended for research and analytical applications. IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis. | ||||||||||||||||||||
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References
- [1]. Moon JA, et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43. [Content Brief]
- [2]. Park CY, 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. [Content Brief]
