New Small Molecules from MCE for June 2020

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.

Compound Screening Libraries

32 specific libraries for high throughput screening (HTS) and high content screening (HCS). Optimized for drug screening and new indication research.

DC-5163 is a potent glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with an IC₅₀ of 176.3 nM and a K_d of 3.192 μM. DC-5163 can inhibit glycolysis pathway partially. DC-5163 also selectively inhibits cancer cell proliferation and induces apoptosis.

Cell Signaling Pathway

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).

1. Nature. 2020 Apr;580(7803):386-390.
2. Nature. 2020 Mar;579(7799):433-437.
3. Science. 2020 Feb 14;367(6479):806-810.
4. Cell. 2020 Mar 5;180(5):941-955.e20.

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.

LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).