MMH409

MMH409 inhibits purified HDAC8 protein with an IC₅₀ of 23.4 nmol/L, adopting a predominantly cis conformation in solution that favors stable binding to the enzyme^[1].
MMH409 (0.000244-1 μM; 10 μM) potently inhibits human HDAC8 with an IC₅₀ of 23.4 nM and exhibits 410-fold selectivity for HDAC8 over other human HDAC isoforms in an enzymatic EMSA^[2].
MMH409 inhibits human HDAC8 with an IC₅₀ of 0.11 μM in a competition-based FP assay^[2].
MMH409 binds full-length human HDAC8 with high affinity, exhibiting a K_D of 3.5 nM in an SPR assay^[2].
MMH409 has high predicted cellular permeability (-log P_e = 5.42) and a human plasma half-life of 93 minutes^[2].
MMH409 (1-10 μM; 90-120 min) potently inhibits purified hHDAC8 protein with an IC₅₀ of 28 nM^[3].
MMH409 (1-10 μM; 90-120 min) weakly inhibits purified SmHDAC8 protein with an IC₅₀ of 11.64 μM, showing a 415.7-fold loss in potency relative to hHDAC8^[3].
MMH409 (50 μM (PAMPA), 1 μM (plasma stability); 16 h (PAMPA), 0-60 min (plasma stability)) has good cell permeability (-log P_e < 6) and human plasma stability (T_1/2 > 1.5 h)^[3].

MMH409 does not exhibit a measurable IC₅₀ for inhibition of colony formation in human neuroblastoma BE(2)-C cells in a colony assay^[2].

MMH409 (10 μM; 72 h) reduces viability of S. mansoni NTS by 18.75%^[3].