LMK-235 is a potent HDAC inhibitor, and is used in cancer research.

HDAC5:4.2 nM, HDAC4:11.9 nM

LMK-235对乳腺肿瘤细胞系MDA-MB-231,舌癌细胞系Cal27和食道癌细胞系Kyse510表现出高细胞毒性,并明显增强顺铂的细胞毒性。此外,LMK-235也对多种疟原虫生命周期阶段表现出纳摩尔级的活性。LMK-235在对顺铂化合物敏感性不同的人癌细胞系中引起HDAC抑制,IC50 <1 μM。

HDAC IC50 Profiling: The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company's standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds.

The rate of cell survival under the action of test substances is evaluated by an improved MTT assay. The assay is based on the ability of viable cells to metabolize yellow MTT to violet formazan that can be detected spectrophotometrically. In brief, A2780, Cal27, Kyse510, and MDA-MB-231 cell lines are seeded at a density of 5000, 7000, 8000, and 10 000 cells/well in 96-well plates. After 24 h, cells are exposed to increased concentrations of the test compounds. Incubation is ended after 72 h, and cell survival is determined by addition of MTT solution (5 mg/mL in phosphate buffered saline). The formazan precipitate is dissolved in DMSO. Absorbance s measured at 544 and 690 nm in a FLUOstar microplate reader. (Only for Reference)