MRT68921-dihydrochloride - ULK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMRT68921 dihydrochlorideCat. No.: HY-100006ACAS No.: 2080306-21-2分式: CHClNO分量: 471.04作靶点: ULK作通路: Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 10 mg/mL (21.23 mM; Need ultrasonic

2、 and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1230 mL 10.6148 mL 21.2296 mL5 mM 0.4246 mL 2.1230 mL 4.2459 mL10 mM 0.2123 mL 1.0615 mL 2.1230 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MRT68921 dihydrochloride是ULK1 和 ULK2 最有效的抑制剂，IC50 值分别为 2.9 nM和 1.1 nM

3、。体外研究ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibitsULK1 and ULK2 in vitro and block autophagy in cells. MRT68921 is the most potent inhibitor of both ULK1and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nm) and gr

4、eater than a 30-foldreduction for ULK2 (1.1 nm). Autophagy-inhibiting capacity of the compounds is specifically through ULK1.ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK11/2 Master of Small Molecules 您边的抑制剂师www.MedChemEin the maturatio

5、n of autophagosomes as well as initiation 1.PROTOCOLKinase Assay 1 Kinase assays are carried out in 50 mM Tris-HCl, pH 7.4, 10 mM magnesium acetate, 0.1 mM EGTA, and0.1% -mercaptoethanol, containing 30 M cold ATP, and 0.5 Ci of -32PATP for 5 min at 25 C. Prior toATP addition, reaction mixes are pre-

6、warmed to 25 C for 5 min. Reactions are stopped by the addition ofsample buffer, followed by SDS, transfer to nitrocellulose, and analysis by autoradiography andimmunoblot 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 MEFs and 293T cell

7、s are grown in DMEM, supplemented with 10% fetal bovine serum andpenicillin/streptomycin, and cultured at 37C, 5% CO2. For induction of autophagy, cells are typically grownto 75% confluency, ished twice, and incubated in Earles balanced salt solution (EBSS) for 1 h (or completemedium as a control).

8、MRT67307 (10 M), MRT68921 (1 M), AZD8055 (1 M), or bafilomycin A1 (50 nM) isincluded 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Biochem J. 2019 Mar 12;476(5):875-887.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. JBiol Chem. 2015 May 1;290(18):11376-83.McePdfHeightCaution: Product has not been fully validated for medical app