124030

Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2

The Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2, N-(2-(Diethylamino)ethyl)-3-(4-((4-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl)methyl)phenyl)-2-phenyl-6-quinolinecarboxamide, 3HCl, N-(2-(Diethylamino)ethyl)-2-(4-((4-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl)methyl)phenyl)-3-phe
• Empirical Formula (Hill Notation): C₄₀H₄₃N₇O₂ · 3HCl
• Molecular Weight: 763.20
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (mixture of regioisomers, HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: yellow
• solubility: DMSO: 25 mg/mL; water: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

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.

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

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable