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PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
DC-5163 is a potent glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with an IC50 of 176.3 nM and a Kd of 3.192 μM. DC-5163 can inhibit glycolysis pathway partially. DC-5163 also selectively inhibits cancer cell proliferation and induces apoptosis.
ONO-7475 is a potent, selective, and orally active novel Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. ONO-7475 sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. ONO-7475 combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.
