化合物Nexturastat A T1819

Product Introduction
Bioactivity


英文名: Nexturastat A

描述: Nexturastat A 是一种有效且特异性的 HDAC6 抑制剂，IC50: 5 nM。它的选择性是其他 HDAC 的 190 倍以上。

细胞实验: B16 murine melanoma cells are plated at 5000/well in 96 well flat bottom plates. The following day, media is changed to that containing various concentrations of HDACi or matched DMSO vehicle concentrations diluted in complete medium done in triplicate. Cells are incubated for 48 hours at 37°C and 5% CO2. Density of viable, metabolically active cells is quantified using a standard MTS assay as per manufacturer’s instructions. Briefly, 20μL of reagent are added per well and incubated at 37°C for 3 hours. Absorbances at 490 nM are measured spectrophotometrically with background subtraction at 690 nM. All values are then normalized and expressed as a percentage of medium control (100%). (Only for Reference)

激酶实验: HDAC inhibition assays: HDAC inhibition assays are performed by Reaction Biology Corp. using isolated human, recombinant full2length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide,RHKKAc, derived from residues 379-382 of p53 is used as substrate. The reaction buffer is made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds are delivered in DMSO and delivered to enzyme mixture with preincubation of 5-10 min followed by substrate addition and incubation for 2 h at 30°C. Trichostatin A and developer are added to quench the reaction and generate fluorescence, respectively. Dose-response curves are generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. IC50 values are then generated from the resulting plots, and the values expressed are the average of duplicate trials ± standard deviation.

体内活性: Nexturastat A对B16鼠黑色素瘤细胞的生长有显著抑制作用（GI50：14.3 μM）。在B16鼠黑色素瘤细胞中,Nexturastat A剂量依赖性增加乙酰化的α-微管蛋白水平,但不影响组蛋白H3乙酰化伴随的脓肿。

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

溶解度: DMSO : 63 mg/mL (184.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (5.85 mM)


关键字: inhibit | HDAC | Histone deacetylases | Inhibitor | Nexturastat A

相关产品: Phenylethyl isothiocyanate | ITSA-1 | Curcumin | Ivaltinostat | HDAC-IN-59 | BML-210 | Suprastat | LMK-235 | TMP195 | HDAC6-IN-25

相关库: Anti-Aging Compound Library | NF-κB Signaling Compound Library | Cancer Cell Differentiation Compound Library | Inhibitor Library | Highly Selective Inhibitor Library | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Histone Modification Compound Library

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