|N-(3-((5-环丙基-2-((2-甲基-1,2,3,4-四氢异喹啉-6-基)氨基)嘧啶-4-基)氨基)丙基)环丁烷甲酰胺盐酸盐|CsnPharm

CAS No.: 2070014-87-6

N-(3-((5-Cyclopropyl-2-((2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)amino)pyrimidin-4-yl)amino)propyl)cyclobutanecarboxamide hydrochloride Catalog No. CSN18901

Synonyms: MRT68921 HCl

MRT68921 HCl is a selective inhibitor of ULK1 and ULK2 with IC50 0f 2.9 nM and 1.1 nM.

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技术信息

生物活性

描述ULK1 (unc-51-like kinase 1), a serine/threonine protein kinase, is essential for the initial stages of autophagy and can be targeted to block autophagy for disease therapy^[2]. MRT68921 hydrochloride 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)^[2]. In line with the in vitro IC₅₀ values, 1 μM MRT68921 was sufficient to reduce phospho-ATG13 which was used as a measure of ULK1 activity to control levels. Therefore, this compound could reduce ULK1 activity in cells. Importantly, it also blocked autophagy as indicated by LC3-II levels^[2].
参考文献

[1] Petherick KJ, Conway OJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 Nov 27;290(48):28726.
[2] Petherick KJ, Conway OJ, Mpamhanga C, Osborne SA, Kamal A, Saxty B, Ganley IG. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. doi: 10.1074/jbc.C114.627778. Epub 2015 Apr 1. Erratum in: J Biol Chem. 2015 Nov 27;290(48):28726. PMID: 25833948; PMCID: PMC4416842.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1230 mL
- 10.6149 mL
- 21.2297 mL
- 5 mM
- 0.4246 mL
- 2.1230 mL
- 4.2459 mL
- 10 mM
- 0.2123 mL
- 1.0615 mL
- 2.1230 mL

技术信息

CAS号

2070014-87-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H35ClN6O

运输

蓝冰

分子量

471.04

别名

MRT68921 HCl

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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N-(3-((5-Cyclopropyl-2-((2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)amino)pyrimidin-4-yl)amino)propyl)cyclobutanecarboxamide hydrochloride Catalog No. CSN18901

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