MRT68921 hydrochloride

• CAT Number: I005769
• Molecular Formula: C25H35ClN6O
• Molecular Weight: 471.04
• Purity: ≥95%
• Target: ULK
• Solubility: H2O: ＞ 31mg/mL
• Storage: Store at -20°C
• IC50: 2.9/1.1 nM (ULK1/2)

MRT68921 hydrochloride 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). 


in vitro: MRT68921 potently inhibits ULK1 and ULK2 and block autophagy in cells. MRT68921 specifically blocks autophagic flux through ULK1 inhibition. MRT68921 is able to inhibit the WT-restored ATG13 phosphorylation and autophagy similarly to cells expressing endogenous ULK1.

Reference

[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 Nov 27;290(48):28726.