5.32384
PI3K Inhibitor, HS-173
Synonym(s):
PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C21H18N4O4S
CAS Number:
Molecular Weight:
422.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥96% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
assay
≥96% (HPLC)
Quality Level
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)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5.32384.0001 | 04055977287226 |