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124030

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C40H43N7O2 · 3HCl
Molecular Weight:
763.20
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Md Naushad Akhtar et al.
PLoS pathogens, 16(12), e1009136-e1009136 (2020-12-29)
The level of CD40 expression on dendritic cells (DCs) plays a decisive role in disease protection during Leishmania donovani (LD) infection. However, current understanding of the molecular regulation of CD40 expression remains elusive. Using molecular, cellular and functional approaches, we

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