5.32384

PI3K Inhibitor, HS-173

• Synonyme(s) : PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
• Formule empirique (notation de Hill): C₂₁H₁₈N₄O₄S
• Numéro CAS: 1276110-06-5
• Poids moléculaire : 422.46
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥96% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 800 pM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: light beige
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: −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
• Clé InChI: SEKOTFCHZNXZMM-UHFFFAOYSA-N

Description

Description générale

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

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PI3Ka

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable