220485 Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem

220485
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₅H₁₃N₅O₂724708-21-8

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220485-500UG
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      Plastic ampoule 500 μg
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      Description
      OverviewA cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory properties. Acts as a potent inhibitor of Chk2 (IC50 = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC50 = 89 nM, 237 nM, 1.352 µM, 2.539 µM, 3.381 µM, and > 10.0 µM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC50 = 3.55 µM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 µM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI50 = 1.73 µM).
      Catalogue Number220485
      Brand Family Calbiochem®
      Synonyms5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one, Chk1 Inhibitor II, Chk2 Inhibitor I
      References
      ReferencesSharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
      Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.
      Product Information
      CAS number724708-21-8
      ATP CompetitiveY
      DeclarationSold under license from Michigan State University.
      FormPale yellow solid
      Hill FormulaC₁₅H₁₃N₅O₂
      Chemical formulaC₁₅H₁₃N₅O₂
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetChk2
      Primary Target IC<sub>50</sub>8 nM against 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 Shipped with Blue Ice or with Dry Ice
      Toxicity Carcinogenic / Teratogenic
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      220485

      References

      Reference overview
      Sharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
      Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.
      Data Sheet

      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
      Synonyms5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one, Chk1 Inhibitor II, Chk2 Inhibitor I
      DescriptionA cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory properties. Acts as a potent inhibitor of Chk2 (IC50 = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC50 = 89 nM, 237 nM, 1.352 µM, 2.539 µM, 3.381 µM, and > 10.0 µM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC50 = 3.55 µM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 µM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI50 = 1.73 µM).
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number724708-21-8
      Chemical formulaC₁₅H₁₃N₅O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Carcinogenic / Teratogenic
      ReferencesSharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
      Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.

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