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504043 Rho Inhibitor II, Y16 - CAS 429653-73-6 - Calbiochem

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CAS #Empirical Formula
429653-73-6C₂₄H₂₀N₂O₃

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      Description
      OverviewA cell-permeable pyrazolidinedione compound that is shown to target RhoGEF DH-PH domain junction with high affinity (Kd = 65 nM) and effetively prevent RhoGEFs LARG, p115, and PDZ from interacting with RhoA, while displaying little potency against DBL-RhoA, LBC-RhoA, intersectin-Cdc42, or TrioN-Cdc42 interaction. Shown to completely prevent serum-induced activation of cellular RhoA, but not Cdc42 or Rac1, in NIH-3T3 cultures (10 µM) and RhoA downstream signaling events. Greatly synergizes with Rho GEF-binding domain blocker Rhosin (Cat. No. 555460) in blocking RhoA-LARG interaction and in preventing cellular RhoA activation (both drug at 5 µM).
      Catalogue Number504043
      Brand Family Calbiochem®
      SynonymsLARG Rho-Binding Domain Blocker, (E)-4-(3-(3-Methylbenzyloxy)benzylidene)-1-phenylpyrazolidine-3,5-dione, (4E)-4-(3-(3-Methylbenzyloxy)benzylidene)-1-phenyl-3,5-pyrazolidinedione, p115 Rho-Binding Domain Blocker, PDZ Rho-Binding Domain Blocker
      References
      ReferencesShang, X., et al. 2013. Proc. Natl. Acad. Sci. USA. 110, 3155.
      Product Information
      CAS number429653-73-6
      FormOrange powder
      Hill FormulaC₂₄H₂₀N₂O₃
      Chemical formulaC₂₄H₂₀N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetRhoGEF
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Número de referencia GTIN
      5.04043.0001 04055977264258