General description
A cell-permeable, allosteric, trisubstituted dihydropyrazolyl compound that acts as a potent, selective, reversible and non-competitive inhibitor of Cdc42 GTPases (IC50 = 0.2, 2.6 and 5.4 µM against nucleotide depleted Cdc42-wt, Cdc42-wt and Cdc42 activated mutant, respectively) with excellent selectivity over Rho family GTPases (IC50 >100 µM for Ras-wt, Ras activated mutant, Rab7-wt, Rab2a-wt, Rac1-wt and Rac1 activated mutant). Shown to efficiently block Cdc42 association with GTPγS and PAK-PBD, and decrease GTP-Cdc42 (>95%) and GTP-Rac1 (≥40%) contents in EGF-stimulated 3T3 cells, and inhibit Bradykinin (Cat. No. 05-23-0500)-induced filopodia formation in 3T3 cells at 10 µM.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Hong, L., et al. 2012. J. Biol. Chem.in press.
Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.2010 Feb 27. (http://www.ncbi.nlm.nih.gov/books/NBK51965/)
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 217708-25MG
