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217692 CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
383907-43-5C₁₅H₁₆ClN₃O₃

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217692-5MG
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      Description
      OverviewA cell-permeable 7-substituted quinolinedione compound that displays antiproliferative properties. Acts as a potent, irreversible and mixed competitive inhibitor of the CDC25 phosphatase family (Ki = 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; IC50 = 210 nM for CDC25B2) and displays nearly 20- and 450-fold greater selectivity for the CDC252 phosphatases over VHR and PTP1B (IC50 = 4.0 µM and > 100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation and delay tumor growth (IC50 = ~1.5 µM in NCI-60 tumor cell panel). Shown to modify CDC25A catalytic domain and to block cellular ERK dephosphorylation in HeLa-CDC25A cells.
      Catalogue Number217692
      Brand Family Calbiochem®
      Synonyms6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione, DA3003-1, PTP Inhibitor XXI, VHR Inhibitor II
      References
      ReferencesChao, J. I., et al. 2004. J. Biol. Chem. 279, 20267.
      Han, Y., et al. 2004. J. Pharmacol. Exp. Ther. 309, 64.
      Pu, L., et al. 2002. J. Biol. Chem. 277, 46877.
      Lazo, J.S., et al. 2001. J. Med. Chem. 44, 4042.
      Product Information
      CAS number383907-43-5
      ATP CompetitiveN
      FormRed solid
      Hill FormulaC₁₅H₁₆ClN₃O₃
      Chemical formulaC₁₅H₁₆ClN₃O₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetCD25A
      Primary Target K<sub>i</sub>29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; 210 nM for CDC25B2
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Carcinogenic / Teratogenic
      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). DMSO stock solutions are stable for up to 1 month at -20°C. Ethanol stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      217692-5MG 04055977202298