产品详情
简单介绍：
MRT68921,AutophagyKinaseULK1/2Inhibitor
详情介绍：
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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