Activators & Inhibitors

Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.

XL-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (HSP90) that selectively inhibits HSP90α and HSP90β with IC50s of 22 nM and 44 nM respectively. It also exerts considerably weaker inhibition against a range of other diverse kinases with IC50 more than 3600 nM for all. In recent studies, XL-888 has exhibits strong anti-proliferative activities in a panel of tumor cells with values of IC50 ranging from 0.1 nM to 45.5 nM.

XL-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (HSP90) that selectively inhibits HSP90α and HSP90β with IC50s of 22 nM and 44 nM respectively. It also exerts considerably weaker inhibition against a range of other diverse kinases with IC50 more than 3600 nM for all. In recent studies, XL-888 has exhibits strong anti-proliferative activities in a panel of tumor cells with values of IC50 ranging from 0.1 nM to 45.5 nM.

XL-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (HSP90) that selectively inhibits HSP90α and HSP90β with IC50s of 22 nM and 44 nM respectively. It also exerts considerably weaker inhibition against a range of other diverse kinases with IC50 more than 3600 nM for all. In recent studies, XL-888 has exhibits strong anti-proliferative activities in a panel of tumor cells with values of IC50 ranging from 0.1 nM to 45.5 nM.

EPZ015666 is a potent, selective, competitive PRMT5 inhibitor (IC50 = 22 nM). EPZ015666 exhibits >10,000-fold specificity for PRMT5 vs. other methyltransferases. EPZ015666 blocks the association of PRMT5 with methylosome protein 50 (WDR77), which is necessary to form an active methyltransferase complex. Treatment of MCL cell lines with nM concentrations of EPZ015666 leads to inhibition of SmD3 methylation and cell death."

EPZ015666 is a potent, selective, competitive PRMT5 inhibitor (IC50 = 22 nM). EPZ015666 exhibits >10,000-fold specificity for PRMT5 vs. other methyltransferases. EPZ015666 blocks the association of PRMT5 with methylosome protein 50 (WDR77), which is necessary to form an active methyltransferase complex. Treatment of MCL cell lines with nM concentrations of EPZ015666 leads to inhibition of SmD3 methylation and cell death."

Guanosine 5'-triphosphate sodium salt hydrate (GTP) functions as a carrier of phosphates and pyrophosphates involved in channeling chemical energy into specific biosynthetic pathways.

Guanosine 5'-triphosphate sodium salt hydrate (GTP) functions as a carrier of phosphates and pyrophosphates involved in channeling chemical energy into specific biosynthetic pathways.

3-aminobenzamide is a novel, potent inhibitor of PARP. Also acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.