General description

A highly cell-permeable and water soluble analog of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124018) that acts as a plecktrin homology (PH)-domain dependent, non-ATP competitive and an allosteric inhibitor of Akt1/2 (IC₅₀ = 560 nM, 390 nM and 7.8 µM in in vitro kinase assay; 526 nM, 730 nM and >10 µM in LNCaP cells for Akt1, Akt2 and Akt3, respectively) with ~ 80-fold greater selectivity over PKA, PKC and SGK (IC₅₀ >50 µM). One of its potent regioisomers (C7-substituted) is shown to enhance induced caspase-3 activity in several tumor cells.

A highly cell-permeable and water soluble analog of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124018) that acts as a plecktrin homology (PH)-domain dependent, non-ATP competitive and an allosteric inhibitor of Akt1/2 (IC₅₀ = 560 nM, 390 nM and 7.8 µM in in vitro kinase assay; 526 nM, 730 nM and >10 µM in LNCaP cells for Akt1, Akt2 and Akt3, respectively) with ~ 80-fold greater selectivity over PKA, PKC and SGK (IC₅₀ >50 µM). One of its potent regioisomers (C7-substituted) is shown to enhance induced caspase-3 activity in several tumor cells.

Legal Information

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

Other Notes

Zhao, Z., et al. 2008. Bioorg. Med. Chem. Lett.18, 49.

Packaging

Packaged under inert gas

2 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)