Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Resminostat hydrochloride (RAS2410 hydrochloride) 是HDAC1,HHDAC3和HDAC6抑制剂,IC50值分别为 42.5、50.1和71.8 nM,对 HDAC8 的活性较低,IC50值为 877 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 285 | 现货 | ||
5 mg | ¥ 836 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 2,930 | 现货 | ||
50 mg | ¥ 4,360 | 现货 | ||
100 mg | ¥ 6,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 836 | 现货 |
产品描述 | Resminostat hydrochloride (RAS2410 hydrochloride) is an effective inhibitor of HDAC1/HDAC3/HDAC6 (IC50: 42.5/50.1/71.8 nM), respectively, and shows less potent activities against HDAC8 (IC50: 877 nM). |
靶点活性 | HDAC6:71.8 nM, HDAC8:877 nM, HDAC1:42.5 nM, HDAC3:50.1 nM |
体外活性 | Resminostat hydrochloride (5 μM) induces histone acetylation in myeloma cells. Resminostat hydrochloride has a substrate competitive binding mode (Ki: 27 nM). Resminostat hydrochloride (5 μM) induces histone hyperacetylation in myeloma cells. Resminostat inhibits cell growth, induces apoptosis and inhibits MM cell proliferation. Resminostat (5 μM) also modulates expression of bcl-2 family proteins and inhibits Akt pathway signalling downstream of Akt. Resminostat inhibits cell growth in head and neck squamous cell carcinoma cell lines (IC50 for SCC25: 0.775 μM; CAL27: 1.572 μM; and FaDu: 0.899 μM). Resminostat (1.25/2.5 μM) has a synergistic effect with irradiation on HNSCC cell lines. Resminostat in combination with cisplatin induces a downregulation of survivin. However, Resminostat shows no effect on Mcl-1 and p-AKT expression. Resminostat reduces viability of HCC cells with the co-therapy of AZD-2014, (IC50s: 0.07-0.89 μM). |
激酶实验 | Forty microliter enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6 or 8 activity, 29 μL enzyme buffer and 1 μL resminostat [HCl] at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30 μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10 μM for HDAC6 and 25 μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 180 min (HDAC1, HDAC6, HDAC8) or 120 min (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/mL trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a Wallac Victor2 1420 multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the 50% inhibitory concentration (IC50) values the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) are set at 0% enzymatic activity (background fluorescence substracted). |
细胞实验 | Resminostat is dissolved in DMSO.A CCK-8 cell proliferation assay is used to investigate the antiproliferative effect of resminostat on HNSCC cells. Cells are seeded into 96-well plates at a density of 3 × 105/well. After 24 hours of growth, the cells are treated with resminostat and cisplatin, either alone or in combination and incubated for 72 hours. Untreated cells maintained in RPMI and equal concentrations of dimethylsulfoxide served as control. After 72 hours, cell proliferation is measured by CCK-8. |
别名 | 4SC-201 hydrochloride, RAS2410 hydrochloride |
分子量 | 385.86 |
分子式 | C16H20ClN3O4S |
CAS No. | 1187075-34-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Resminostat hydrochloride 1187075-34-8 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Resminostat Hydrochloride RAS-2410 4SC-201 hydrochloride 4SC 201 Hydrochloride 4SC201 Hydrochloride RAS-2410 Hydrochloride RAS 2410 Hydrochloride Resminostat 4SC-201 Histone deacetylases Inhibitor RAS2410 hydrochloride RAS 2410 inhibit RAS2410 Hydrochloride 4SC-201 Hydrochloride RAS2410 inhibitor