Extremely potent KV1.3 channel blocker (Kd = 23 pM for mKV1.3 currents). Selective for KV1.3 over other mammalian potassium channels (IC50 values are 23, 1800, 10500, 37000 and 39000 pM for mKV1.3, mKV1.1, hKV1.6, mKV1.4 and rKV1.2 respectively, and >1000
AP-22161 selectively binds the Src SH2 domain by targeting highly conserved phosphotyrosine binding to cysteine residues in the pocket. AP-22161 selectively inhibits Src SH2 binding and can be used to inhibit osteoclast absorption.
BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.
SLUPP-225 is an efflux pump inhibitor (EPI) by interacting with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli.