5.32384

PI3K Inhibitor, HS-173

• Synonym(e): PI3K Inhibitor, HS-173, PI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
• Empirische Formel (Hill-System): C₂₁H₁₈N₄O₄S
• CAS-Nummer: 1276110-06-5
• Molekulargewicht: 422.46
• MDL-Nummer: MFCD28023584
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥96% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: 800 pM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light beige
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: −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
• InChIKey: SEKOTFCHZNXZMM-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Primary Target
PI3Ka

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable