5.32384
PI3K Inhibitor, HS-173
别名:
PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
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关于此项目
经验公式（希尔记法）:
C21H18N4O4S
化学文摘社编号:
分子量:
422.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥96% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥96% (HPLC)
Quality Segment
form
powder
potency
800 pM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light beige
solubility
DMSO: 50 mg/mL
storage temp.
−20°C
SMILES string
[S](=O)(=O)(Nc2cncc(c2)c3c[n]4c(ncc4C(=O)OCC)cc3)c1ccccc1
InChI
1S/C21H18N4O4S/c1-2-29-21(26)19-13-23-20-9-8-15(14-25(19)20)16-10-17(12-22-11-16)24-30(27,28)18-6-4-3-5-7-18/h3-14,24H,2H2,1H3
InChI key
SEKOTFCHZNXZMM-UHFFFAOYSA-N
General description
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
PI3Ka
Preparation Note
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.
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
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable