BTdCPU is an activator of HRI (heme-regulated eIF2α kinase) with anticancer activity. It can promote eIF2α phosphorylation and induced apoptosis in resistant cells. The eIF2-alpha kinase HRI is a novel therapeutic target in multiple myeloma. Combination therapy with rapamycin, an mTOR inhibitor, and BTdCPU, an activator of HRI, demonstrated additive effects on apoptosis in dex-resistant […]

GSK2656157 (GSK-2656157) is a novel, potent, ATP-competitive and highly selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) enzyme with IC50 of 0.9 nM in cell-free assays, it has 500-fold greater activity against a panel of 300 kinases.

ISRIB, the trans-isomer of ISRIB, is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with IC50 of 5 nM.

Salubrinal is a novel, potent, cell-permeable and selective inhibitor of eIF2α (eukaryotic translation initiation factor 2 subunit α) dephosphorylation with potential anticancer activity.

GSK2606414 is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.