MRT68921 HCl

SKU: orb1301858

Description

MRT68921 hydrochloride is a highly potent dual inhibitor of the autophagy-initiating kinases ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. This compound is a valuable research tool for investigating autophagy mechanisms in both cellular and animal models of cancer and neurodegenerative diseases.

Research Area

Cell Biology, Immunology & Inflammation, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2070014-87-6
• MW: 471.04
• Purity: 99.98% (May vary between batches)
• Formula: C₂₅H₃₄N₆O·HCl
• SMILES: Cl.CN1CCc2cc(Nc3ncc(C4CC4)c(NCCCNC(=O)C4CCC4)n3)ccc2C1
• Target: ROS,GSK-3,Bcl-2 Family,Apoptosis,Autophagy
• Solubility: DMSO:4.72 mg/mL (10.02 mM);H2O:10 mg/mL (21.23 mM)

Bioactivity

• Target IC50:
  ULK1:2.9 nM|ULK2:1.1 nM
• In Vitro:
  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). MRT68921 (1 μM) was sufficient to reduce phospho-ATG13 to control levels, and in line with the in vitro IC50 values . Pre-incubating the cells for 30 min with the ULK1 inhibitor MRT68921 at the optimal concentration of 100 nM prevented the forskolin-induced CYTO-ID staining. The same effect was observed with siRNA against ULK1 .
• Cell Research:
  Immortalized wild-type mouse embryonic fibroblasts (MEFs) have been described previously. MEFs and 293T cells were grown in DMEM, supplemented with 10% fetal bovine serum and penicillin/streptomycin, and cultured at 37 °C, 5% CO2. For induction of autophagy, cells were typically grown to 75% confluency, washed twice, and incubated in Earle's balanced salt solution (EBSS) for 1 h (or complete medium as a control) unless indicated. MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) was included where indicated. Transfection and transduction were as described .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MRT68921 HCl, MRT-68921 HCl, ULK1, ULK2

Compound Identifiers

PubChem CID

121230974