MRT68921 HCl
作者：齐岳
发布时间：2023-09-13
17:24:15
点击数：
产品名称：MRT68921 HCl
产品描述：
| 产品描述 | MRT68921 hydrochloride is a potent inhibitor of both ULK1 and ULK2 (IC50s: 2.9 and 1.1 nM, respectively). |
| 靶点活性 | ULK2:1.1 nM, ULK1:2.9 nM |
| 体外活性 | MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nM) and greater than a 30-fold reduction for ULK2 (1.1 nM). MRT68921 (1 μM) was sufficient to reduce phospho-ATG13 to control levels, and in line with the in vitro IC50 values [1]. Pre-incubating the cells for 30 min with the ULK1 inhibitor MRT68921 at the optimal concentration of 100 nM prevented the forskolin-induced CYTO-ID staining. The same effect was observed with siRNA against ULK1 [2]. |
| 激酶实验 | Initial ULK1 kinase assays were performed with GST-ULK1, produced in Sf9 cells. For other experiments, recombinant GST-ULK1 (wild type, kinase-dead (K46I), and M92T and M92Q) was expressed in 293T cells, purified, and eluted from a glutathione-Sepharose column. Kinase assays were carried out in 50 mM Tris-HCl, pH 7.4, 10 mM magnesium acetate, 0.1 mM EGTA, and 0.1% β-mercaptoethanol, containing 30 μM cold ATP, and 0.5 μCi of [γ-32P]ATP for 5 min at 25 °C. Prior to ATP addition, reaction mixes were prewarmed to 25 °C for 5 min. Reactions were stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot. For IC50 curve measurements, kinase assays were performed, using myelin basic protein as a substrate [1]. |
| 细胞实验 | Immortalized wild-type mouse embryonic fibroblasts (MEFs) have been described previously. MEFs and 293T cells were grown in DMEM, supplemented with 10% fetal bovine serum and penicillin/streptomycin, and cultured at 37 °C, 5% CO2. For induction of autophagy, cells were typically grown to 75% confluency, washed twice, and incubated in Earle's balanced salt solution (EBSS) for 1 h (or complete medium as a control) unless indicated. MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) was included where indicated. Transfection and transduction were as described [1]. |
| 别名 | 盐酸MRT68921 |
| 分子量 | 471.04 |
| 分子式 | C25H34N6O·HCl |
| CAS No. | 2070014-87-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 10 mg/mL
H2O: 10 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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