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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。
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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 | 库存 | 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 x 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能够以相近的效力抑制WT和突变型EZH2的甲基转移酶活性。在七种DLBCL细胞系的研究中,GSK503显示出对细胞生长的抑制作用,并且这种效果在与ABT737或Obatoclax联用时得到增强。[1] |
体内活性 | 在接种SRBC的C57BL6小鼠中,GSK503(150 mg/kg,i.p.)降低了脾细胞中的H3K27me3水平。在携带SUDHL4和SUDHL6肿瘤的雄性SCID小鼠中,GSK503(150 mg/kg,i.p.)抑制了肿瘤生长。[1] 在携带鼠B16-F10肿瘤的C57Bl/6小鼠中,GSK503(150 mg/kg,i.p.)显著降低了全身H3K27me3水平,抑制了肿瘤生长,并几乎消除了转移形成。[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 |
Smiles | CC(C)n1cc(C)c2c(cc(cc12)-c1ccc(nc1)N1CCN(C)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O |
密度 | 1.24 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 93 mg/mL (176.6 mM) Ethanol: 25 mg/mL (47.5 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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