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Merck
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重要文件

220486

Sigma-Aldrich

Chk2 Inhibitor II

Chk2 Inhibitor II, BML-277, CAS 516480-79-8 is a cell-permeable, potent, reversible, ATP-competitive inhibitor of Chk2 (IC₅₀ = 15 nM).

同義詞:

Chk2 Inhibitor II, 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide

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About This Item

經驗公式(希爾表示法):
C20H14ClN3O2
CAS號碼:
分子量::
363.80
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥95% (HPLC)

形狀

solid

效力

15 nM IC50

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

pale yellow

溶解度

DMSO: 5 mg/mL

運輸包裝

ambient

儲存溫度

2-8°C

SMILES 字串

Clc1ccc(cc1)Oc2ccc(cc2)c3[nH]c4c(n3)cc(cc4)C(=O)N

InChI

1S/C20H14ClN3O2/c21-14-4-8-16(9-5-14)26-15-6-1-12(2-7-15)20-23-17-10-3-13(19(22)25)11-18(17)24-20/h1-11H,(H2,22,25)(H,23,24)

InChI 密鑰

UXGJAOIJSROTTN-UHFFFAOYSA-N

一般說明

A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC50 of 15 nM and a Ki of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC50 = 12 M and 17 M, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 M), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC50 of 3 M and 7.6 M, respectively. Also available as a 25 mM solution in DMSO (Cat. No. 220491).

生化/生理作用

Cell permeable: yes
Ki = 37 nM inhibiting Chk2.EC50 = 3 µM and 7.6 µM in rescuing both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis
Primary Target
Chk2
Product competes with ATP.
Reversible: yes
Target Ki: 37 nM inhibiting Chk2

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他說明

Arienti, K. L., et al. 2005. J. Med. Chem.48, 1873.

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3


分析證明 (COA)

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