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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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, p115 Rho-Binding Domain Blocker, PDZ Rho-Binding Domain Blocker

Primary Target: RhoGEF
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504043
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
429653-73-6C₂₄H₂₀N₂O₃

Products

Catalog NumberPackaging Qty/Pack
5.04043.0001 Glass bottle 10 mg
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
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
Global Trade Item Number
Catalog Number GTIN
5.04043.0001 04055977264258

Documentation

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

Title

Safety Data Sheet (SDS) 

Rho Inhibitor II, Y16 - CAS 429653-73-6 - Calbiochem Certificates of Analysis

TitleLot Number
504043

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
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
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
CAS number429653-73-6
Chemical formulaC₂₄H₂₀N₂O₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
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.