WT161 is a potent and selective inhibitor of HDAC6 (IC50:0.40 nM).

HDAC6:0.40 nM

将抗多发性骨髓瘤（MM）细胞系用WT161处理可比tubacin更有效地引起乙酰化微管蛋白的积累和MM细胞系的细胞死亡。此外，WT161与BTZ联合应用可在体外[1]诱导协同增强的细胞毒性，并克服BTZ的耐药性。

WT161 在小鼠异种移植模型中显著抑制了 MCF7 细胞的体内生长，这与 ERα 的下调有关[2]。

Female NCr nu/nu mice were subcutaneously (sc) implanted with 17?-estradiol-sustained release pellets (0.18 mg, 60 day release time). Mice were inoculated sc with 5 × 10^6 MCF-7 cells suspended in 30% Matrigel. After 1 month of growth, mice with measurable tumors (> 50 mm^3) were assigned into cohorts receiving intraperitoneal WT161 daily (80 mg/kg) or into a control group receiving vehicle alone (10% DMSO, 90% PBS). Caliper measurements of the longest perpendicular tumor diameters were performed every alternate day to estimate the tumor volume, using the formula volume = ? x L x W^2. Animals were sacrificed when tumors reached 2 cm or if the mice appeared moribund. For each animal, relative tumor volume was determined by normalizing data to the baseline tumor volume for that animal at the start of treatment. Statistical significance was determined by 2-way ANOVA analysis[2].