Bioactivity | MRT68921 hydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. |
Invitro | ULK1 是一种丝氨酸/苏氨酸蛋白激酶,对于自噬的初始阶段至关重要。MRT68921 在体外抑制 ULK1 和 ULK2,并阻断细胞中的自噬。MRT68921 是 ULK1 和 ULK2 的最有效抑制剂,ULK1 (2.9 nm) 的 IC50 降低超过 15 倍,ULK2 (1.1 nm) 的 IC50 降低超过 30 倍。该化合物的自噬抑制能力具体是通过 ULK1 实现的。ULK1 抑制会导致停滞的早期自噬体结构积累,表明 ULK1 在自噬体成熟和启动中发挥作用[1]。 0 --> MRT68921 hydrochloride 相关抗体: |
Name | MRT68921 hydrochloride |
CAS | 2070014-87-6 |
Formula | C25H35ClN6O |
Molar Mass | 471.04 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |