LAQ824 (Dacinostat) 化学構造
分子量: 379.459

品質と確認

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製品情報

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    HDAC阻害剤を比較
  • 研究分野

製品の説明

生物活性

情報 LAQ824 (Dacinostat)は、32nMのIC50による新しいHDAC阻害剤です。
目標 HDAC
IC50 32 nM [1]
In vitro試験 LAQ824 activates the expression of the gene encoding the p21 cell cycle inhibitor by activating the p21 promoter with 50% of the maximal promoter activation (AC50) of 0.30 μM. LAQ824 inhibits the cell growth of both H1299, a non-small cell lung carcinoma line, and HCT116, a colon cancer cell line with IC50 of 0.15 μM and 0.01 μM, respectively, and the antiproliferative effect of LAQ824 is selective toward the tumor cell lines while inducing only growth arrest in normal fibroblasts. Furthermore, LAQ824 induces a dose-dependent increase of p21 protein in A549 cells and an increase in the hypophosphorylated state of the Rb tumor suppressor. [1] A recent study shows that LAQ824 induces chromatin changes at the level of the IL-10 gene promoter that lead to enhanced recruitment of the transcriptional repressors HDAC11 and PU.1 and inhibits IL-10 production in BALB/c murine macrophages. [2]
In vivo試験 In HCT116 and human colon tumor xenografts in nude mice, LAQ824 treatment at 100 mg/kg produces the inhibitory effects on tumor growth in a dose-dependent mode without general cytotoxicity. [1]
臨床試験
特集

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

細胞系 H1299, HCT116, DU145, PC3 and MDA435 cells
濃度 0-10 μM
処理時間 48 hours
方法 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 X0, %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.

動物実験: [1]

動物モデル HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
製剤 LAQ824 is dissolved in DMSO.
投薬量 ≤100 mg/kg
管理 Administered via i.v.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

参考

化学情報

Download LAQ824 (Dacinostat) SDF
分子量 379.459
化学式

C22H25N3O3

CAS No. 404951-53-7
保管 2年-20℃
6月-80℃in DMSO
別名 NVP-LAQ824
溶解度 (25°C) * In vitro DMSO 76 mg/mL (200 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (E)-3-(4-(((2-(1H-indol-3-yl)ethyl)(2-hydroxyethyl)amino)methyl)phenyl)-N-hydroxyacrylamide

研究分野

カスタマーレビュー (4)


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Rating
Source Molecular Pain , 2010, 6, 51. LAQ824 (Dacinostat) purchased from Selleck
Method Paw withdrawal latency analysis
Cell Lines C57BL/6NTac mice
Concentrations 8-200 ng
Incubation Time 30 min
Results CFA-induced thermal hyperalgesia was significantly attenuated by all HDACIs, except for MS-275, in comparison to vehicle. Of these tested HDACIs, LAQ824 showed similar inhibitory effects between 40 and 200 ng suggesting saturation above 40 ng dosage.

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Rating
Source Diabetologia, 2012, 55(9), 2421-31.. LAQ824 (Dacinostat) purchased from Selleck
Method Cell viability assay
Cell Lines INS-1 cells
Concentrations 16-80 h
Incubation Time
Results CI-994, PCI24781 and LAQ824 all protected against cytokine-induced beta cell death, whereas the HDAC8-selective inhibitor PCI34051 showed no protection.

Click to enlarge
Rating
Source Diabetologia, 2012, 55, 2421–2431. LAQ824 (Dacinostat) purchased from Selleck
Method Analyses of efficacy, potency and IC50
Cell Lines INS-1 cells
Concentrations
Incubation Time
Results HC toxin, CI-994, PCI24781 and LAQ824 all protected against cytokine-induced beta cell death, whereas the HDAC8-selective inhibitor PCI34051 showed no protection.

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Rating
Source Dr. Zhang of Tianjin Medical University. LAQ824 (Dacinostat) purchased from Selleck
Method Western blot
Cell Lines
Concentrations 0.01-20 µM
Incubation Time
Results LAQ824 treatment resulted in a reduction of Histone H3 acetylation.

製品表彰状 (3)

技術サポート&よくある質問(FAQ)

顧客がするかもしれない質問に対する答えは、指示を取り扱っている阻害剤で見つかります。話題は、貯蔵液(阻害剤と特別な注意を細胞ベースの分析法と動物のために必要とする問題を保存することは実験します)を準備する方法を含みます。

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