MRT68921 dihydrochloride 是 ULK1 和 ULK2 有效的抑制剂，IC₅₀ 值分别为 2.9 nM和 1.1 nM。

MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC 50 values of 2.9 nM and 1.1 nM, respectively.

Solid

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. has not independently confirmed the accuracy of these methods. They are for reference only. <

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83.

In Vitro: H₂O : 31.25 mg/mL (61.58 mM; Need ultrasonic)DMSO : 8.33 mg/mL (16.41 mM; ultrasonic and warming and heat to 60°C)配制储备液