CP-100356 is a specific inhibitor of MDR1 (P-Gp), the protypical ABC transporter. The compound has low uM to nM potency for inhibiting several MDR-1 substrates (calcein-AM, digoxin) in transfected MDCKII cells. CP-100356 also inhibits prazosin transport in human breast cancer resistance protein (BCRP)-transfected MDCKII cells, suggesting that it acts as a dual inhibitor. CP-100356 does not inhibit multidrug resistance-associated protein 2 (MPR2 IC50 >15 mM).
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Rho proteins are signalling molecules that control cellular dynamics, movement and morphological changes. They are activated by Rho guanine-nucleotide exchange factors (Rho GEFs) that transduce upstream signals into Rho-mediated activation of downstream processes. Fgd5 is a Rho GEF involved in
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