124036-M

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

Properties

• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2