UNC2250，5MG，SML3620-5MG，Sigma

Biochem/physiol Actions

Potent and highly selective Mer receptor tyrosine kinase (MerTK) inhibitor in vitro and in vivo.
UNC2250 is a potent and highly selective Mer receptor tyrosine kinase inhibitor (MerTK IC50 = 1.7 nM; Tyro3/Axl IC50 = 100/270 nM) that reduces endogenous Mer phosphorylation level (697 B-ALL IC50 = 9.8 nM post 1h treatment) and blocks ligand-stimulated activation of a chimeric EGFR-Mer in cells. UNC2250 inhibits colony-forming potential in rhabdoid (by 36% at 100 nM; BT-12 cells) and NSCLC tumor cells (Colo699 IC50 = 100 nM) with good pharmacokinetic properties. UNC2250 is reported to reduce mortality in a murine LPS-induced acute lung injury (ALI) model (2 mg/kg i.v. )