LY-364947 (396129-53-6) is a selective ALK5 inhibitor, IC50 = 59, 400 and 1400 nM for TGF-β RI, TGF-β RII and MLK-7K, respectively.1 Inhibits Smad2 phosphorylation induced by TGF-β as well as fibronectin expression and MDA-MB-231 cell invasion.2 LY-364947 abolishes resistance of glioblastoma-initiating cells to radiation.3 Cell permeable.
References/Citations:
1) Sawyer et al. (2003), Synthesis and activity of new aryl-and hetero-aryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain; J. Med. Chem., 46 3953 2) Shiou et al. (2006), Smad4-dependent regulation of urokinase plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-beta; J. Biol. Chem., 281 33971 3) Hardee et al. (2012), Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β; Cancer Res., 72 4119
CAS:
396129-53-6
Catalog Number:
10-1492
Activity:
ALK5 inhibitor
Alternate Names:
HTS-466284
Chemical Name:
4-(3-Pyridin-2-yl-1H-pyrazol-4-yl)quinolone
Molecular Weight:
272.31
Molecular Formula:
C17H12N4 Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Brown solid
Purity:
98% by TLC
Storage Temperature:
RT (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT