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Merck
CN
所有图片(1)

主要文件

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.

别名:

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

经验公式(希尔记法):
C40H43N7O2 · 3HCl
分子量:
763.20
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

方案

≥97% (mixture of regioisomers, HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

颜色

yellow

溶解性

DMSO: 25 mg/mL
water: 50 mg/mL

运输

ambient

储存温度

2-8°C

一般描述

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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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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