Tacedinaline (CI994) is a selective class I HDAC inhibitor with potential antineoplastic activity.

HDAC2:0.9 μM, HDAC3:1.2 μM, HDAC1:0.9 μM

在耐化疗的胰腺导管癌小鼠,和人前列腺肿瘤模型中,CI-994均表现出抗肿瘤活性.

CI-994具有抗肿瘤活性,并且在实体肿瘤中表现出更高的细胞毒作用。在多种细胞中,CI-994抑制细胞生长,如大鼠白血病BCLO细胞（IC50=2.5 μM）,LNCaP细胞（IC50=7.4 μM）。在A-549和LX-1细胞中,CI-994（< 160 mM ）使细胞在G0/G1期增加,S期减少,能够抑制细胞生长,并且诱导细胞凋亡。

LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×104) are seeded in 24-well plates and incubated in a 5% CO2 incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate. (Only for Reference)