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Alternative_name
2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide
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Description
A cell-permeable, potent, and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2; IC₅₀ = 15 nM; Ki = 37 nM). Displays ~1,000-fold greater selectivity for Chk2 compared to Cdk1/cyclin B and CK1 (IC₅₀ = 12 µM and 17 µM, respectively) and only weakly affects the activities of a panel of 31 kinases (< 25% inhibition at 10 µM), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC₅₀ of 3 µM and 7.6 µM, respectively.
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CAS Number
516480-79-8
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₀H₁₄CIN₃O₂
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Molecular Weight
363.8
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Cell Permeable
Yes
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Purity
≥98% by HPLC
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Solubilities
DMSO (10 mg/ml)
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Handling
Protect from air and moisture
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Tag Line
A Chk2 inhibitor
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
12 months
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MDL Number
MFCD08276917
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PubChem CID
9969021
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SMILES
C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl
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InChi
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)
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InChi Key
UXGJAOIJSROTTN-UHFFFAOYSA-N
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MSDS Available
Yes
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
