LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research.
LSD1-IN-24 (compound 3S)(0-20 μM, 5 days) can reduce PD-L1 levels in an LSD1-dependent manner and enhance the T cell killing response of BGC-823 cells in a dose-dependent manner, but does not affect BGC -823 and MFC cell proliferation. Furthermore, it dose-dependently protects H3K4me1/2 but not H3K4me3 from demetlation[1].
LSD1-IN-24 (compound 3S) (0-50 mg/kg, oral gavage; daily for 2 weeks) inhibits in vivo MFC cell growth, tumor weight in a dose-dependent manner in a subcutaneous tumor model containing MFC cells Significantly decreased, tumor tissue Ki67 decreased significantly, and no obvious toxic effect on mice[1].
References:
[1]. Xing-Jie Dai, et al. Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells. J Med Chem. 2023 Mar 23;66(6):3896-3916.