MRT68921

MRT68921 is a potent NUAK1/ULK1 dual inhibitor. MRT68921 inhibits ULK1 and ULK2 with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. MRT68921 can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 can be used for the research of cancer, such as breast cancer^[1][2]. IC50 & Target:IC50: 2.9 nM (ULK1), 1.1 nM(ULK2)^[1] In Vitro:MRT68921 (1 μM, 1 h) reduces basal LC3 puncta and blocks basal autophagy in mouse embryonic fibroblasts (MEFs)^[1].
MRT68921 (1 μM) reduces LC3-II levels in TBK1 knock-out and matched wild-type MEFs^[1].
MRT68921 (24 h) exhibits cytotoxic activity in cancer cells with IC₅₀ values ranging from 1.76-8.91 μM^[2].
MRT68921 (0-10 μM, 8-24 h) induces ROS production and apoptosis in NCI-H460 and MNK45 cells^[2].
MRT68921 (0-5 μM, 8h) suppresses the NUAK1/MYPT1/Gsk3β andautophagy associated signaling pathway in U251 and MNK45 cells^[2].
In Vivo:MRT68921 (10-40 mg/kg, s.c., daily for 7 times) inhibits tumor growth in NCI-H460 tumor mice models^[2].
MRT68921 (20 mg/kg, s.c., every 2 days for 7 times) inhibits tumor growth in MNK45 tumor mice models^[2].
MRT68921 (20 mg/kg, i.p., daily for 7 times) reduces the number of lung metastatic nodules in 4T1 tumor mice models^[2].