New from SYNkinase for April
3 New Kinases and 5 Non-Kinase inhibitors


mTOR inhibitor, PP242 (SYN-1181).

PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively.

Other mTOR inhibitors from Synkinase: AZD2014, AZD8055, INK128, KU0063794


Potent Pim inhibitor, CX6258 (SYN-1182)

CX6258 was reported to be the potent inhibitors of Pim-1, Pim-2 and Pim-3 kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM, respectively.

Other Pim inhibitors from Synkinase: SMI-4a

Potent TRK inhibitor, GNF-5837 (SYN-1183)

GNF-5837 is a potent, selective and orally bioavailable pan-TRK inhibitor of TRKA, TRKB and TRKC with the IC50 of 11nM, 9nM and 7nM, respectively.

Other TRK inhibitors from Synkinase: GW441756


New Non-Kinase Inhibitors
 

Ombrabulin inhibited tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells.
  

GANT61 is a GLI antagonist that inhibits GLI1 and GLI2-induced transcription with IC50 of 5 μM. It also inhibit the hedgehog (Hh) signaling pathway downstream of SMO and SUFU causing GLI1 nuclear accumulation.

 
  PF-8380 (SYN-3005) A potent autotaxin inhibitor 

PF-8380 is a potent inhibitor of autotaxin (IC₅₀ = 2.8 nM in an in vitro enzyme assay). It inhibits autotaxin activity in human whole blood (IC₅₀ = 101 nM).