MRT68921 hydrochloride

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Chemical Structure| 2070014-87-6 同义名 : MRT68921 HCl
CAS号 : 2070014-87-6
货号 : A695028
分子式 : C25H35ClN6O
纯度 : 99%+
分子量 : 471.038
MDL号 : MFCD30187515
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Autophagy

    ULK1, IC50:2.9 nM

    ULK2, IC50:1.1 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.23mL

4.25mL

2.12mL
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.