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124036-M

Millipore

Akt Inhibitor XVIII, SC66

The Akt Inhibitor XVIII, SC66 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Akt Inhibitor XVIII, SC66, (2 E,6 E)-2,6- bis(4-Pyridylmethylene)cyclohexanone, (2E,6E)-2,6-bis(4-Pyridylmethylene)cyclohexanone

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About This Item

Empirical Formula (Hill Notation):
C18H16N2O
Molecular Weight:
276.33
UNSPSC Code:
12352200

Quality Level

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 25 mg/mL

storage temp.

2-8°C

General description

A cell-permeable pyridine compound that represses Akt activation by allosterically disrupting Akt-PH domain binding to PIP3 and directly facilitating Akt ubiquitination with little proteasomal or deubiquitination activity. Blocks phosphorylations of Akt-Ser473 and downstream targets TSC, FOXO and PRAS40 in HEK293T cells at 8 µg/ml with minimal effect on pAkt-Thr450. Shown to be highly efficacious towards PI 3-K inhibitor resistant Akt1-E17K mutant and exert synergistic apoptotic activity with LY 294002 (Cat. No. 440202) against HeLa cells. Suppresses tumor growth in a mouse HEK293T-xenograft model (30 mg/kg, s.c., twice per week).
A cell-permeable pyridine compound that selectively targets Akt, but not PLCδ, PH domain, preventing Akt membrane localization/activation and rendering Akt in a conformation susceptible to ubiquitination and subsequent proteasomal degradation. Akti-1/2 (Cat. Nos. 124017 & 124018) competes for Akt PH domain binding and blocks SC66-induced Akt ubiquitination and proteasomal degradation. Effectively inhibits HEK293T growth both in vitro (>99 inhibition at 0.4 M) and in mice in vivo (84% of control tumor size with twice weekly i.p. dose of 30 mg/kg), Synergizes with LY294002 (Cat. Nos. 440202 & 440204) in cell death induction in HeLa and HS-Sultan cultures in vitro.

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Jo, H., et al. 2011. Proc. Natl. Acad. Sci. USA108, 6486.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2


Certificates of Analysis (COA)

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