Dacinostat
作者：齊岳
發(fā)布時間：2023-09-12
09:04:41
點擊數(shù)：
產(chǎn)品名稱：Dacinostat
產(chǎn)品描述：
| 產(chǎn)品描述 | LAQ824 (Dacinostat) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter. |
| 靶點活性 | HDAC:32 nM |
| 體外活性 | 100 mg/kg LAQ824劑量依賴性抑制攜帶HCT116和人結腸*移植瘤的裸鼠生長,且無細胞毒性. |
| 體內活性 | LAQ824誘導A549細胞中p21蛋白的劑量依賴性增加和Rb抑制因子的低磷酸化狀態(tài)的增加。LAQ824在IL-10基因啟動子水平誘導染色質改變,導致增強的轉錄抑制因子HDAC11和PU.1的募集并抑制BALB/c鼠巨噬細胞中IL-10的產(chǎn)生。此外,LAQ824通過激活p21啟動子,也激活編碼p21細胞周期抑制劑的基因表達,大啟動子活性AC50為50%時,濃度為0.30 μM。 LAQ824抑制H1299（一種非小細胞肺*細胞系）和HCT116（一種結腸*細胞系）的細胞生長,IC50分別為0.15 μM和0.01 μM,LAQ824的抗增殖作用對細胞系具有選擇性,同時僅在正常成纖維細胞中誘導生長停滯。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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 X<T0, %Growth=(X-T0)/T0*100; If X>T0, %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) |
| 別名 | 達西司特, LAQ824, NVP-LAQ824 |
| 分子量 | 379.46 |
| 分子式 | C22H25N3O3 |
| CAS No. | 404951-53-7 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
H2O: <1 mg/mL
DMSO: 71 mg/mL (187.1 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯(lián)系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業(yè)務范圍包括化學試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產(chǎn)品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯(lián)劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
