生物活性
GSK343是有效的组蛋白H3-赖氨酸27（H3K27）甲基转移酶EZH2抑制剂（IC = 4 nM）。对除EZH1以外的其他HMT的选择性是1000倍（选择性是60倍）。GSK343抑制HCC1806细胞中的H3K27甲基化，IC小于200nM（通过免疫荧光测量）。
靶点信息
| EZH2 (Cell-free assay) | EZH1 (Cell-free assay) | | | |
| 4 nM | 240 nM | | | |
化学数据
| 目录号 | A13114 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 541.69 |
| Formula | C31H39N7O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1346704-33-3 |
| Synonyms | GSK-343, GSK 343 |
| SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C |
溶解度
| In vitro | DMSO | Warmed: 1 mg/mL (1.84 mM) |
| Water | Insoluble |
| Ethanol | 3 mg/mL (5.54 mM) |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 18.46 mL | 92.3 mL | 184.61 mL |
| 0.5 mM | 3.69 mL | 18.46 mL | 36.92 mL |
| 1 mM | 1.85 mL | 9.23 mL | 18.46 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.69 mL |
*The above data is based on the productmolecular weight 541.69. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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