MARK4 inhibitor 1 is a potent inhibitor of microtubule affinity-regulated kinase 4 (MARK4) with an IC50 value of 1.54±0.22μM against MARK4. MARK4 has been found to be overexpressed in multiple cancer types, making it a potential target for cancer prevention or treatment interventions. MARK4 inhibitor 1 can bind to the active site residues of MARK4, inhibiting cell migration, promoting apoptosis and enhancing ROS generation. In vitro experiments, MARK4 inhibitor 1 was not toxic to wild-type HEK293 cells, but its IC50 values against MARK4-overexpressing HepG2, MDA-MB-435s and MCF-7 cells were 6.22±1.11μM, 9.94±1.12μM, and 8.14±1.10μM, respectively[1].
References:
[1] Aneja B, Khan NS, Khan P, et al. Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis. Eur J Med Chem. 2019;163:840-852.
MARK4 inhibitor 1是微管亲和力调节激酶4（MARK4）的强效抑制剂，对MARK4的IC50值为1.54±0.22μM。MARK4在多种癌症类型中过度表达，是癌症预防或治疗干预措施的潜在靶点。MARK4 inhibitor 1能够与MARK4的活性位点残基结合，抑制细胞迁移，促进细胞凋亡，增强ROS生成。体外实验中，MARK4 inhibitor 1对野生型HEK293细胞无毒性，但对过表达MARK4的HepG2、MDA-MB-435s和MCF-7细胞的IC50值分别为6.22±1.11μM、9.94±1.12μM和8.14±1.10μM[1]。