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220486 Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem

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

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide

Primary Target: Chk2
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220486
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Tableau de caractéristiques principal

CAS #Empirical Formula
516480-79-8C₂₀H₁₄ClN₃O₂

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220486-1MG
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      Description
      OverviewA 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 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. Also available as a 25 mM solution in DMSO (Cat. No. 220491).
      Catalogue Number220486
      Brand Family Calbiochem®
      Synonyms2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide
      References
      ReferencesArienti, K. L., et al. 2005. J. Med. Chem. 48, 1873.
      Product Information
      CAS number516480-79-8
      ATP CompetitiveY
      FormPale yellow solid
      Hill FormulaC₂₀H₁₄ClN₃O₂
      Chemical formulaC₂₀H₁₄ClN₃O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetChk2
      Primary Target IC<sub>50</sub>15 nM; 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 K<sub>i</sub>37 nM inhibiting Chk2
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      220486-1MG 04055977201147

      Documentation

      Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      220486

      Références bibliographiques

      Aperçu de la référence bibliographique
      Arienti, K. L., et al. 2005. J. Med. Chem. 48, 1873.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision16-December-2009 RFH
      Synonyms2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide
      DescriptionA cell-permeable, potent, reversible 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.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number516480-79-8
      Chemical formulaC₂₀H₁₄ClN₃O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesArienti, K. L., et al. 2005. J. Med. Chem. 48, 1873.

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      Catégories

      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Cell Cycle/Cell Division > Checkpoint Kinase Inhibitors