CCT020312-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECCT020312Cat. No.: HY-119240CAS No.: 324759-76-4分式: CHBrNO分量: 650.4作靶點: PERK作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (192.19 mM; Need ultrasonic)H2O : 40% P

2、EG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.20 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.20 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.20 mM); Clear solution1/2 Master of Small Mol

3、ecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 CCT020312是選擇性的 EIF2AK3/PERK 的激活劑。CCT020312 可誘導細胞細胞中 EIF2A 的磷酸化。IC50 & Target EIF2AK3/PERK 1 2.體外研究 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

4、6.1 M 1.CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durablerather than transient cytostasis 1.Treatment of HT29 cells with 10 M CCT020312

5、 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 p27KIP1present in such cells 1.體內(nèi)研究 Treatment of 15-week-old wildtype mice with the PERK activator CCT020312 (1-5 mg/kg; i.p.; once daily for3 da

6、ys) leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates 2.P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performessignificantly better in Morris water maze 2.Animal Model: 9-week-old P301S tau transgenic mice 2Dosage: 2 mg/kgAdministra

7、tion: Intraperitoneal injection; once daily for 6 weeksResult: P301S transgenic mice treated with CCT020312 performed significantly better in Morriswater maze.REFERENCES1. Stockwell SR, et al.Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling.PLoS One. 2012;7(1):e28568.2. Bruch J, et al. PERK activation mitigates tau pathology in vitro and in vivo. EMBO Mol Med. 2017 Mar;9(3):371-384.McePdfHeightCaution: Product has not been fully validated for medical applications.For re