Description
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.
Product information
CAS Number: 1190378-57-4
Molecular Weight: 464.60
Formula: C26H36N6O2
Chemical Name: N-(3-((5-cyclopropyl-2-((3-(morpholinomethyl)phenyl)amino)pyrimidin-4-yl)amino)propyl)cyclobutanecarboxamide
Smiles: O=C(NCCCNC1=NC(NC2=CC(CN3CCOCC3)=CC=C2)=NC=C1C1CC1)C1CCC1
InChiKey: UKBGBACORPRCGG-UHFFFAOYSA-N
InChi: InChI=1S/C26H36N6O2/c33-25(21-5-2-6-21)28-11-3-10-27-24-23(20-8-9-20)17-29-26(31-24)30-22-7-1-4-19(16-22)18-32-12-14-34-15-13-32/h1,4,7,16-17,20-21H,2-3,5-6,8-15,18H2,(H,28,33)(H2,27,29,30,31)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
MRT68921 was usually used at 1 µM final concentration in vitro.
References:
- 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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