达西司特 T2454

Product Introduction
Bioactivity


英文名: Dacinostat

描述: Dacinostat (NVP-LAQ824) 是一种新型 HDAC 抑制剂，IC50 为 32 nM，是 p21 启动子的激活剂。它也可抑制HDAC1的活性，IC50值为 9 nM，主要用于癌症研究。

细胞实验: Cell proliferation is measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay). The cells are seeded in 12-well dishes and cultured in RPMI 1640 containing 10% FBS. The cells are cultured in the presence of various concentrations of TSA (up to 1,000 ng/mL). To examine the growth inhibition by TSA, viable cell numbers are determined by trypan blue dye exclusion, counted in a Nesbauer-type hemocytometer for 0 hour, 24 hours, and 48 hours. The same amount of ethanol is added to the RPMI 1640 medium as the control experiment. All experiments are performed in duplicate and repeated 3 times The average background value (treatment with medium alone) is subtracted from each experimental well; triplicate values are averaged for each compound dilution. The following formulas are used to calculate the percentage of growth: If XT0, %Growth=(X-T0)/(GC-T0)*100. where T0 is the average value of T0 ? background, GC is the average value of untreated cells (in triplicate) ? background, and X is the average value of compound-treated cells (in triplicate)-background. The "% Growth" is plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.(Only for Reference)

激酶实验: In Vitro Histone Deacetylase Assay: HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl2, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO4, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-32P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.

体外活性: 100 mg/kg LAQ824剂量依赖性抑制携带HCT116和人结肠癌移植瘤的裸鼠肿瘤生长,且无细胞毒性.

体内活性: LAQ824诱导A549细胞中p21蛋白的剂量依赖性增加和Rb肿瘤抑制因子的低磷酸化状态的增加。LAQ824在IL-10基因启动子水平诱导染色质改变,导致增强的转录抑制因子HDAC11和PU.1的募集并抑制BALB/c鼠巨噬细胞中IL-10的产生。此外,LAQ824通过激活p21启动子,也激活编码p21细胞周期抑制剂的基因表达,最大启动子活性AC50为50%时,浓度为0.30 μM。 LAQ824抑制H1299（一种非小细胞肺癌细胞系）和HCT116（一种结肠癌细胞系）的细胞生长,IC50分别为0.15 μM和0.01 μM,LAQ824的抗增殖作用对肿瘤细胞系具有选择性,同时仅在正常成纤维细胞中诱导生长停滞。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 71 mg/mL (187.1 mM)


关键字: LAQ 824 | LAQ-824 | NVP-LAQ 824 | NVP-LAQ-824 | Histone deacetylases | inhibit | Autophagy | HDAC | Inhibitor | Dacinostat

相关产品: ITF3756 | ACY-1083 | RG2833 | Pracinostat | Divalproex Sodium | Entinostat | HDAC8-IN-20a | BRD 9757 | HDAC-IN-59 | CXD101

相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Autophagy Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途