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Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.

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Probe Reports from the NIH Molecular Libraries Program [Internet].

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Figure 2. CID2950007 is a Non-Competitive Inhibitor of Cdc42.

Figure 2CID2950007 is a Non-Competitive Inhibitor of Cdc42

Equilibrium binding studies were performed with 3–100 nM BODIPY-FL-GTP and wild type Cdc42 plus 10 μM CID 2950007 (triangles) or DMSO vehicle (squares) with either (A) 1 mM EDTA or (B) 1 mM Mg2+ ions. In (C) BODIPY-FL-GTP was tested from 10 nM to 1 μM in the presence of Mg2+ ions using 10 μM CID2950007 and nucleotide-depleted Cdc42. The principal mode of action is a decrease in GTP binding sites (Bmax) rather than a change in GTP affinity. In (D), IC50 for CID 2950007 (squares) of 200 nM was determined using nucleotide-depleted Cdc42, 1 mM Mg2+ ions and 1.5 nM BODIPY-FL-GTP. A related analog CID 2971684 had IC50 = 400 nM (triangles) in this assay.

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