达西司特|T2454|TargetMol

Dacinostat
404951-53-7

￥477 1mg 起订

￥691 2mg 起订

￥1110 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 达西司特

英文名称：: Dacinostat

CAS号：: 404951-53-7

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 95.28%

产品类别：: 抑制剂

货号：: T2454

Product Introduction

Bioactivity

名称	Dacinostat
描述	LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.
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 \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 40 mg/mL (105.42 mM), Sonication is recommended.
关键字	LAQ 824 \| LAQ-824 \| NVP-LAQ 824 \| NVP-LAQ-824 \| Histone deacetylases \| inhibit \| Autophagy \| HDAC \| Inhibitor \| Dacinostat
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相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| ReFRAME 相关化合物库 \| 抗衰老化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 人代谢物化合物库 \| 抗癌药物库

达西司特|||NVP-LAQ824|||LAQ824|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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