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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C10H8ClNO
CAS Number:
28755-03-5
Molecular Weight:
193.63
UNSPSC Code:
12352200
MDL number:
MFCD00464796
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, desiccated, protect from light

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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

100

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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