CI994 是一种组蛋白脱乙酰酶抑制剂,抑制重组 HDAC 1, 2 和 3 的IC50值分别为 0.9,0.9,1.2 μM。
产品描述
Tacedinaline (CI994) is a selective class I HDAC inhibitor with potential antineoplastic activity.
体外活性
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.
体内活性
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。
细胞实验
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)
Cas No.
112522-64-2
分子式
C15H15N3O2
分子量
269.304
别名
CI994;N-acetyldinaline;PD-123654;Goe-5549;Acetyldinaline
储存和溶解度
DMSO:26.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years