CCT020312 (CCT-020312) is a small molecule PERK activator, inhibits pRB phosphorylation in HT29 colon carcinoma cells with EC50 of 5.1 uM.
CCT020312 shows no effect on the activity on CDK4/cyclin D or CDK1/cyclin B, effectively inhibits cell proliferation of HT29 colon carcinoma cells with IC50 of 3.1 uM (96 h).
CCT020312 elicits EIF2A phosphorylation in cells, does not induce full ER stress signalling; also reduced tau phosphorylation, tau conformational change and 4-repeat tau isoforms, and increased cell viability in cultured human neurons.
CCT020312 significantly improved memory and locomotor function, reduced tau pathology, and prevented dendritic spine and motoneuron loss in P301S tau mice.
