124037

Akt Inhibitor XIX, 3CAI

The Akt Inhibitor XIX, 3CAI, also referenced under CAS 28755-03-5, controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Akt Inhibitor XIX, 3CAI, 3-Chloroacetyl-indole, 2-Chloro-1-(1H-indol-3-yl)ethanone
• Empirical Formula (Hill Notation): C₁₀H₈ClNO
• CAS Number: 28755-03-5
• Molecular Weight: 193.63
• MDL number: MFCD00464796

Properties

• Quality Level: 100
• 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
• 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

Description

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.

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. Effectively inhibits Akt-mediated downstream effector proteins phosphorylation 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 in mice (EC₅₀ = 30 mg/kg; 5 times/wk for 3 wks via p.o.) in vivo.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3