MR24 TFA, a G-5555 derivative, is a mammalian STE20-like ( MST ) kinase inhibitor. MR24 TFA shows selectively to MST3/4 over MST1/2, with EC 50 values of 57 and 583 nM, respectively. MR24 TFA induces G1 phase cell cycle arrest. MR24 TFA can be used for cancer research, such as breast, liver and lung cancers [1].
In Vitro, MR24 (compound 24) (1-10 μM, 6-72 h) TFA shows no significant effect on cell healthy nuclei in HCT116 cells, and only results in a slight reduction in cell viability by about 30% at a concentration of 10 μM[1]. MR24 (1-10 μM, 24-72 h) TFA induces G1 phase cell cycle arrest in HCT116 cells[1].
References:
[1]. Rak M, et al. Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors. J Med Chem. 2024 Mar 14;67(5):3813-3842.
In Vitro, MR24 (compound 24) (1-10 μM, 6-72 h) TFA shows no significant effect on cell healthy nuclei in HCT116 cells, and only results in a slight reduction in cell viability by about 30% at a concentration of 10 μM[1]. MR24 (1-10 μM, 24-72 h) TFA induces G1 phase cell cycle arrest in HCT116 cells[1].
References:
[1]. Rak M, et al. Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors. J Med Chem. 2024 Mar 14;67(5):3813-3842.