A cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC50 = 800 pM). Blocks the proliferation of several cancer cells (IC50 = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).
PI3 K alpha inhibitor; anti-fibrolytic agent; HS-173
Biochem/physiol Actions
Cell permeable: yes
Primary Target PI3Ka
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Son, M.K., et al. 2013. Sci. Rep.3, 3470.
Lee, H., et al. 2013. Onc. Rep.30, 863. Kim, O., et al. 2011. J. Med. Chem.54, 2455.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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