Key Specifications Table
Pricing & Availability
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|5.04043.0001||Glass bottle||10 mg||
|Overview||A 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).|
|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|
|References||Shang, X., et al. 2013. Proc. Natl. Acad. Sci. USA. 110, 3155.|
|Structure formula Image|
|Purity||≥95% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Shang, X., et al. 2013. Proc. Natl. Acad. Sci. USA. 110, 3155.|
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.