GSK-503CAS号： 1346572-63-1分子式： C31H38N6O2分子量： 526.67描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
GSK503 is a specific EZH2 methyltransferase inhibitor.
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| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
GSK-503,GSK503,GSK 503
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| 外观 |
Powder
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| 可溶性/溶解性 |
DMSO 100 mg/mL (189.87 mM)
Ethanol 26 mg/mL warmed (49.36 mM) |
| 生物活性 | |
| 靶点 |
EZH2
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| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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. 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.
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分子结构图
