MRT-68921

SKU: orb1226846

Description

A potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively; inhibits a number of kinases by over 80% in a broad panel of 80 protein kinases, including TBK1 and AMPK; reduces phospho-ATG13 and blocks autophagy in cells.

Key Properties

• CAS Number: 1190379-70-4
• MW: 434.5771
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₄N₆O
• SMILES: CN1CCC2=C(C1)C=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4CCC4)C5CC5
• Target: ULK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. MRT68921 inhibits ULK1 and ULK2 in vitro and block autophagy in cells. 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). Autophagy-inhibiting capacity of the compounds is specifically through ULK1. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MRT68921 | MRT 68921

Quick Database Links

Gene Symbol

ULK