CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
IC50&Target
EIF2AK3/PERK.
体外研究
Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM.
CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis.
Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells.
体内研究
Treatment of 15-week-old wildtype mice with the PERK activator CCT020312 (1-5 mg/kg; i.p.; once daily for 3 days) leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates.
P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performes significantly better in Morris water maze.
Animal Model:
9-week-old P301S tau transgenic mice
Dosage:
2 mg/kg
Administration:
Intraperitoneal injection; once daily for 6 weeks
Result:
P301S transgenic mice treated with CCT020312 performed significantly better in Morris water maze.
分子式
C31H30Br2N4O2
分子量
650.40
CAS号
324759-76-4
运输条件
Room temperature in continental US; may vary elsewhere.