Description: LMK-235 (LMK235) is a novel, potent and selective inhibitor of HDAC4 and HDAC5 (histone deacetylase) with potential antitumor activity. It inhibits HDAC4/5 with IC50s of 11.9 nM and 4.2 nM, respectively. It has IC50s of 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM for HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, respectively. LMK235 showed similar effects compared to vorinostat on inhibition of cellular HDACs in a pan-HDAC assay but enhanced cytotoxic effects against the human cancer cell lines A2780, Cal27, Kyse510, and MDA-MB231. LMK235 shows nanomolar inhibition of HDAC4 and HDAC5, whereas vorinostat and TSA inhibit HDAC4 and HDAC5 in the higher micromolar range. In contrast to vorinostat, LMK235 showed a novel HDAC isoform selectivity profile with preference for HDAC4 and HDAC5, which are inhibited with low nanomolar IC50 values.
References: J Med Chem. 2013 Jan 24;56(2):427-36; Eur J Med Chem. 2014 Jul 23;82:204-13.
Publications Citing Use of InvivoChem LMK-235: Cancers 2022, 14(18), 4537; https://doi.org/10.3390/cancers14184537