Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 500 nM in blocking the geranyl-geranylation of Rap1A

Cell permeable: yes

Primary TargetGGTase-I

General description

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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Bernot, D., et al. 2003. J. Cardiovasc. Pharmacol.41, 316.Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.

Packaging

Packaged under inert gas

250 µg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)