CCT020312

生物活性靶点体外研究体内研究 CCT020312 试剂级价格

CCT020312

CAS号:324759-76-4
英文名:CCT020312
中文名:CCT020312
CBNumber:CB04844628
分子式:C31H30Br2N4O2
分子量:650.4
MOL File:324759-76-4.mol

CCT020312化学性质

密度 :1.48±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: soluble
形态 :A solid
酸度系数(pKa) :9.43±0.70(Predicted)
颜色 :Light yellow to yellow

CCT020312性质、用途与生产工艺

生物活性 CCT020312 是选择性的 EIF2AK3/PERK 的激活剂。CCT020312 可诱导细胞细胞中 EIF2A 的磷酸化。
靶点

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.