MRT68921, Autophagy Kinase ULK1/2 Inhibitor


Catalog No. size PriceQuantity
M60311-2S 2 mg solid $109
M60311-10S 10mg solid $447

Description

Product Information
Molecular Weight: 464.61
Formula: C26H36N6O2
Purity: ≥98%
CAS#: 1190378-57-4
Solubility: DMSO up to 100 mM
Chemical Name: N-(3-((5-cyclopropyl-2-((3-(morpholinomethyl)phenyl)amino)pyrimidin-4-yl)amino)propyl)cyclobutanecarboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

MRT68921 is a potent, selective and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively. It can inhibit ULK in vitro and block autophagy in cells. By generating the drug-resistant M92T ULK1 mutant, MRT68921demostrates to specifically block autophagic flux through ULK1 inhibition and disrupt autophagosome maturation, not through AMPK-related kinase involvement. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation.

How to Use:


In vitro: MRT68921 was usually used at 1 µM final concentration in vitro.
In vivo: n/a

Reference:

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


 


Products are for research use only. Not for human use. 

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