InChI
1S/C10H8ClNO/c11-5-10(13)8-6-12-9-4-2-1-3-7(8)9/h1-4,6,12H,5H2
InChI key
LLZQFAXTCYDVTR-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated, protect from light
color
pink
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
A cell-permeable chloroacetyl-indole compound that inhibits Akt1 and Akt2 kinase activity (IC50<1 µM) by directly targeting Akt PH domain, exhibiting little or much reduced activity against a panel of 84 other kinases, including PI-3 Kinase (60% inhibition at 10 µM). Effectively inhibits Akt-mediated cellular GSK3β Ser9 and mTOR Ser2448 phosphorylation (4 µM in HCT116 cultures) in a time-dependent manner, resulting in effective apoptosis induction in HCT116 and HT29 cultures (by 55% and 60%, respectively; 4 µM for 4 days). Reported to retard HCT116-derived tumor growth by 50% when administered at an oral dosage of 30 mg/kg in mice (5 times/wk for 3 wks) in vivo.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kim, D.J., et al. 2011. Cancer Prev. Res.4, 1842.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
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