Product does not compete with ATP.
Target IC50: 500 nM in blocking the geranyl-geranylation of Rap1A
Cell permeable: yes
Methyl ester derivative of GGTI-2133 (Cat. No. 345884). A potent and selective non-thiol inhibitor of geranylgeranyltransferase I (GGTase I) over farnesyltransferase (FTase) in whole cells. Blocks the geranylgeranylation of Rap1A with an IC50 value greater than 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50﹤30 µM for H-Ras).
A cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I). Blocks the geranyl-geranylation of Rap1A with an IC50 value that is over 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50 >30 µM for H-Ras).
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Bernot, D., et al. 2003. J. Cardiovasc. Pharmacol.41, 316.Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.
Packaged under inert gas
250 µg in Plastic ampoule
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity: Standard Handling (A)