MRT-68921

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、相对特异性的 ULK1 和 ULK2 抑制剂，IC50 分别为 2.9 和 1.1 nM。

A potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively; inhibits a number of kinases by over 80% in a broad panel of 80 protein kinases, including TBK1 and AMPK; reduces phospho-ATG13 and blocks autophagy in cells.

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.

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MRT68921 | MRT 68921

Autophagy

ULK

ULK1|ULK2

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1190379-70-4

434.5771

C25H34N6O

>98% (HPLC)

10 mM in DMSO

CN1CCC2=C(C1)C=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4CCC4)C5CC5

Cyclobutanecarboxamide, N-[3-[[5-cyclopropyl-2-[(1,2,3,4-tetrahydro-2-methyl-6-isoquinolinyl)amino]-4-pyrimidinyl]amino]propyl]-

(-20℃)

With Ice Pack

≥ 2 years