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

220485
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₃N₅O₂ 724708-21-8

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          Calbiochem Biologics 32.2
          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.