Biochem/physiol Actions

Primary TargetRab7

Reversible: yes

Cell permeable: yes

General description

A thiourea-derived small molecule that acts as a competitive inhibitor of nucleotide (BODIPY-GTP and BODIPY-GDP) binding by Rab7 (K_i = 12.89-19.70 nM). Equilibrates rapidly with Rab7 without affecting the rate of release of bound BODIPY-GTP or BODIPY-GDP. However, it exhibits a slightly lower potency against BODIPY-GDP bound Rab7 than BODIPY-GTP bound Rab7A. Acts by binding to the nucleotide binding pocket of Rab7. Also shown to inhibit nucleotide binding by mutant forms of Rab7 (Rab7Q67L and Rab7T22N) that are constitutively in the GTP and GDP bound states, with good potency. Also shown to block the nucleotide binding of several other Ras-related GTPases, but with reduced potency.

Legal Information

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

Other Notes

Agola, J. O., et al. 2012. ACS Chem Bio.7, 1095.

Packaging

Packaged under inert gas

10 mg in Glass bottle

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)