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Beschreibung

A thiourea-derived small molecule that acts as a competitive inhibitor of nucleotide (BODIPY-GTP and BODIPY-GDP) binding by Rab7 (Ki = 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.