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504043 Rho Inhibitor II, Y16 - Calbiochem

504043
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₀N₂O₃

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      Glass bottle 10 mg
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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®
      Synonymsp115 Rho-Binding Domain Blocker, PDZ Rho-Binding Domain Blocker, LARG 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
      References
      ReferencesShang, X., et al. 2013. Proc. Natl. Acad. Sci. USA. 110, 3155.
      Product Information
      FormOrange powder
      Hill FormulaC₂₄H₂₀N₂O₃
      Chemical formulaC₂₄H₂₀N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetRhoGEF
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Rho Inhibitor II, Y16 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Shang, X., et al. 2013. Proc. Natl. Acad. Sci. USA. 110, 3155.
      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.

      Revision21-June-2013 JSW
      Synonymsp115 Rho-Binding Domain Blocker, PDZ Rho-Binding Domain Blocker, LARG 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
      DescriptionA cell-permeable pyrazolidinedione compound that prevents RhoGEFs LARG, p115, and PDZ from interacting with RhoA, while displaying little potency against DBL-RhoA, LBC-RhoA, intersectin-Cdc42, or TrioN-Cdc42 interaction. Structure and in vitro binding studies using DH-PH domains-containing human LARG catalytic fragment (aa 765-1138) constructs reveals RhoGEF DH-PH domain junction as the high affinity Y16 targeting site (Kd = 65, 472, 2121, and > 5 x 105 nM using wt, K979A, E982A, and N983A LARG, respectively). Shown to prevent serum-induced activation of cellular RhoA, but not Cdc42 or Rac1, in serum-starved NIH-3T3 cultures (215%, 109%, and 87% of basal RhoA-GTP level with 0, 10, or 30 µM Y16, respectively) and effectively inhibit RhoA downstream signaling events, including FAK and MLC phosphorylations and stress fiber formation without apparent cytotoxicity (50 µM up to 24 h) or affecting Cdc42-mediated filapodia and Rac1-mediated lamellipodia formation. Greatly synergizes with Rho GEF-binding domain blocker Rhosin (Cat. No. 555460) in blocking RhoA-LARG binding (8%, 27%, and 72% inhibition, respectively, with 5 µM G04 alone, 5 µM Y16 alone, or in combination) and in inhibiting cellular RhoA activation (80% inhibition of serum-stimulated RhoA-GTP level by 30 µM Y16 alone or by a combination of 5 µM each of G04 and Y16 in serum-starved NIH-3T3 cells).
      FormOrange powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₂₀N₂O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      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 Standard Handling
      ReferencesShang, X., et al. 2013. Proc. Natl. Acad. Sci. USA. 110, 3155.