Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SP2509 是一种选择性 LSD1拮抗剂,IC50值为 13 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 349 | 现货 | ||
5 mg | ¥ 816 | 现货 | ||
10 mg | ¥ 1,320 | 现货 | ||
25 mg | ¥ 2,230 | 现货 | ||
50 mg | ¥ 3,320 | 现货 | ||
100 mg | ¥ 4,850 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 816 | 现货 |
产品描述 | SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM). |
靶点活性 | LSD1:13 nM |
体外活性 | 在负荷OCI-AML3异种移植物的小鼠中,SP2509(25 mg/kg i.p. ),能够抑制肿瘤生长,延迟动物的存活. |
体内活性 | 在OCI-AML3中,SP250能够抑制集落形成,诱导细胞凋亡。在AML细胞中,SP2509能够抑制LSD1与CoREST作用,增加启动子特异性H3K4Me3,同时诱导p53,p21和C/EBPα。在原代AML细胞中,SP2509诱导细胞的增殖。 |
激酶实验 | SP2509 activity assays: Test compounds are diluted to 20 × the desired test concentration in 100% DMSO and 2.5?μL of the diluted drug sampleis added to a black 384-well plate. The LSD1 enzyme stock is diluted 17-fold with assay buffer and 40?μL of the diluted LSD1 enzyme is added to the appropriate wells. Substrate, consisting of horseradish peroxidase, dimethyl K4 peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3, and 10-acetyl-3,7-dihydroxyphenoxazine is then added to wells. Resorufin is analyzed on an Envision plate reader with an excitation wavelength of 530?nm and an emission wavelength of 595?nm. The activity of SP2509 on the other oxidases is determined by using commercially available kits. The glucose oxidase activity (which also noncovalently binds FAD in an elongate conformation), is determined using the glucose oxidase kit. The MAO assays are performed using the MAO-glo kit with MAO-A and MAO-B. |
细胞实验 | Cultured AML cells are treated with SP2509 and/or PS for 96?h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37?°C. Colony formation is measured 7–10 days after plating.(Only for Reference) |
别名 | HCI-2509 |
分子量 | 437.9 |
分子式 | C19H20ClN3O5S |
CAS No. | 1423715-09-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 36 mg/mL (82.2 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2836 mL | 11.4181 mL | 22.8363 mL | 57.0907 mL |
5 mM | 0.4567 mL | 2.2836 mL | 4.5673 mL | 11.4181 mL | |
10 mM | 0.2284 mL | 1.1418 mL | 2.2836 mL | 5.7091 mL | |
20 mM | 0.1142 mL | 0.5709 mL | 1.1418 mL | 2.8545 mL | |
50 mM | 0.0457 mL | 0.2284 mL | 0.4567 mL | 1.1418 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。
SP2509 1423715-09-6 Apoptosis Chromatin/Epigenetic Histone Demethylase HCI 2509 SP 2509 SP-2509 inhibit Inhibitor HCI-2509 HCI2509 inhibitor