324759-76-4
324759-76-4 结构式
基本信息
化合物CCT020312
2(1H)-Quinolinone, 6-bromo-3-[5-(4-bromophenyl)-1-[3-(diethylamino)-1-oxopropyl]-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-
物理化学性质
常见问题列表
EIF2AK3/PERK.
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.
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. |