首页Chromatin/EpigeneticHDACEntinostat
Entinostat
编号 T6233     别名: SNDX-275, MS-275
CAS 209783-80-2     分子式 C21H20N4O3     分子量 376.41
靶点: HDAC1; HDAC3;
Entinostat (MS-275) is an inhibitor of HDACs that inhibits HDAC1 and HDAC3 (IC50s: 0.18/0.74 μM).
纯度:99.20%
规格 库存 单价 数量
10 mg 上海现货 408.00
50 mg 上海现货 917.00
100 mg 上海现货 1392.00
200 mg 待询 2532.00
1 mL * 10 mM (in DMSO) 上海现货 291.00
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生物活性

产品描述

Entinostat (MS-275) is an inhibitor of HDACs that inhibits HDAC1 and HDAC3 (IC50s: 0.18/0.74 μM).

靶点活性

HDAC1,0.51μM

HDAC3,1.7μM

实验溶液

2% DMSO+30% PEG 300: 10mg/mL

体外活性

MS-275通过作用于2′-氨基而抑制HDACs,作用于HDAC1和 HDAC3时IC50 分别为0.51 μM和1.7 μM。而对其他的HDACs(HDAC4, 6, 8和10)没有抑制效果。人类白血病和淋巴癌细胞(U937, HL-60, K562, 和Jurkat)都能够被MS-275有效抑制。MS-275降低cyclin D1、抗凋亡蛋白Mcl-1和XIAP的表达。在K562细胞中,MS-275诱导p21WAF1/CIP1和凝溶胶蛋白的累积。在A2780细胞中,MS-275能够降低S期细胞,提高G1期细胞。在U937细胞中,MS-275可以诱导p21CIP1/WAF1 调节的生长和变异Marker (CD11b)的表达。

体内活性

恶性实体瘤、恶性血液病和畸变基因表达,MS-275均可以起到治疗的作用。肾细胞癌中,MS-275和IL-2联用降低调节性T细胞和增强脾细胞的表达,显示出强抗癌活性。除了HCT-15的人类移植瘤,MS-275(49 mg/kg)都显示出强抗癌活性。

激酶实验

Standard HDAC Assays: Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.

细胞实验

Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration. (Only for Reference)

细胞系: A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells

动物实验

动物模型:A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.

化学信息

分子量

376.41

分子式

C21H20N4O3

CAS

209783-80-2

溶解度

DMSO: 37.6 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.657 ml 13.283 ml 26.567 ml
5 mM 0.531 ml 2.657 ml 5.313 ml
10 mM 0.266 ml 1.328 ml 2.657 ml
50 mM 0.053 ml 0.266 ml 0.531 ml
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