A selective inhibitor of TGF-β RI

LY364947 – 5 mg

Brand:
Cayman
CAS:
396129-53-6
Storage:
-20
UN-No:
Non-Hazardous - /

Transforming growth factor-β (TGF-β) signals through a cell surface heteromeric complex involving type I (TGF-β RI) and type II (TGF-β RII) receptors. Downstream signal transduction is mediated by the TGF-β RI kinase domain through the phosphorylation of Smad proteins. LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC50 value of 59 nM.{17263} LY364947 less effectively inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and mixed-lineage kinase 7 (MLK7; IC50 = 1,400 nM).{17263,17264} It inhibits TGF-β-induced cell growth (IC50 = 89 nM) in NIH 3T3 mouse fibroblasts{17263} and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.{17265}  

 

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Description

A selective inhibitor of TGF-β RI, with an IC50 value of 59 nM; poorly inhibits TGF-β RII (IC50 = 400 nM), p38 MAPK (IC50 = 740 nM), and MLK7 (IC50 = 1,400 nM); inhibits TGF-β-induced cell growth (IC50 = 89 nM) and Smad phosphorylation

Formal name: 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline

Synonyms:  HTS 466284|TGF-β RI Kinase Inhibitor

Molecular weight: 272.3

CAS: 396129-53-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|ALK (Activin-like Kinase) Signaling

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