5.32384

PI3K Inhibitor, HS-173

• Sinônimo(s): PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
• Fórmula empírica (Notação de Hill): C₂₁H₁₈N₄O₄S
• Número CAS: 1276110-06-5
• Peso molecular: 422.46
• Número MDL: MFCD28023584
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥96% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• potência: 800 pM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: light beige
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: [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
• chave InChI: SEKOTFCHZNXZMM-UHFFFAOYSA-N

Descrição

Descrição geral

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

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
PI3Ka

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras 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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable