Featured Inhibitors for October-BOC Sciences

Quizartinib Quizartinib is an orally available small molecule with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. 

PIK-75 PIK-75 was developed as part of a PI 3-kinase drug discovery program. PIK75 attenuates insulin stimulation of Akt/PKB in a range of cell types at 100 nM. The compound has been reported to block growth of a range of cell lines with an IC50 value in the region of 50 nM. In vivo studies have shown that PIK-75, administered at 50 mg/kg, inhibited the growth of HeLa cell xenografts in mice models.

WAY-252623 WAY-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of LXR, which can reduces total serum cholesterol and LDL cholesterol and inhibits lesion growth in models of atherosclerosis. IC50 values= 24 and 179 nM (for LXRβ and LXRα, respectively)

GW3965 GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). In Vitro: Recruit the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay

Cyt387 Cyt387, also called Momelotinib, under the IUPAC name N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide, is an ATP competitive inhibitor of JAK1 (IC50 = 11 nM) and JAK2 (IC50 = 18 nM) with potential antineoplastic activity, which may result result in the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.