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Key Documents

5.32384

Sigma-Aldrich

PI3K Inhibitor, HS-173

Sinónimos:

PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor

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About This Item

Fórmula empírica (notación de Hill):
C21H18N4O4S
Número de CAS:
Peso molecular:
422.46
Código UNSPSC:
12352200
NACRES:
NA.77

Análisis

≥96% (HPLC)

Nivel de calidad

formulario

powder

potencia

800 pM IC50

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

light beige

solubilidad

DMSO: 50 mg/mL

temp. de almacenamiento

−20°C

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

Clave InChI

SEKOTFCHZNXZMM-UHFFFAOYSA-N

Descripción general

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).
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).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
PI3 K alpha inhibitor; anti-fibrolytic agent; HS-173

Acciones bioquímicas o fisiológicas

Cell permeable: yes
Primary Target
PI3Ka

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

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.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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