Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK503是一种高效特异性EZH2甲基转移酶抑制剂,Ki 值为3到27 nM,具有潜在的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,270 | 现货 | ||
50 mg | ¥ 3,480 | 现货 | ||
100 mg | ¥ 4,930 | 现货 | ||
500 mg | ¥ 10,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 859 | 现货 |
产品描述 | GSK-503, a potent EZH2 inhibitor, has potential antitumor activity. |
靶点活性 | EZH2:8 nM |
体外活性 | GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition and the effects are enhanced by ABT737 or Obatoclax. [1] |
体内活性 | In C57BL6 mice immunized with SRBC, GSK503 (150 mg/kg, i.p.) reduced the level of H3K27me3 in splenocytes. In male SCID mice bearing SUDHL4 and SUDHL6 tumors, GSK503 (150 mg/kg, i.p.) inhibits tumor growth. [1] In C57Bl/6 mice bearing murine B16-F10 tumors, GSK503 (150 mg/kg, i.p.) significantly reduces global H3K27me3 levels, inhibits tumor growth and virtually abolishes metastases formation. [2] |
激酶实验 | In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively. |
分子量 | 526.67 |
分子式 | C31H38N6O2 |
CAS No. | 1346572-63-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (176.6 mM)
Ethanol: 25 mg/mL (47.5 mM)
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 / Ethanol | 1 mM | 1.8987 mL | 9.4936 mL | 18.9872 mL | 47.4681 mL |
5 mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | 9.4936 mL | |
10 mM | 0.1899 mL | 0.9494 mL | 1.8987 mL | 4.7468 mL | |
20 mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 2.3734 mL | |
DMSO | 50 mM | 0.038 mL | 0.1899 mL | 0.3797 mL | 0.9494 mL |
100 mM | 0.019 mL | 0.0949 mL | 0.1899 mL | 0.4747 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。
GSK503 1346572-63-1 Chromatin/Epigenetic Histone Methyltransferase Inhibitor inhibit GSK-503 GSK 503 inhibitor