MRT68921, Autophagy Kinase ULK1/2 Inhibitor


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

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:

  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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