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MRT68921 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRT68921 dihydrochloride图片
CAS NO:2080306-21-2
规格:98%
分子量:471.04
包装与价格:
包装价格(元)
1g电议
500mg电议
5mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
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。
CAS:2080306-21-2
分子式:C25H35ClN6O
分子量:471.04
纯度:98%
存储:Store at -20°C

Background:

MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.


ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibits ULK1 and ULK2 in vitro and block autophagy in cells. 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). Autophagy-inhibiting capacity of the compounds is specifically through ULK1. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation[1].



[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83.