MRT-68921

Research use only, not for human use.

A potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively.

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