生物活性
GSK126是一种有效的，高选择性的，具有S-腺苷甲硫氨酸竞争性的小分子EZH2甲基转移酶活性抑制剂，可降低总体H3K27me3水平并重新激活沉默的PRC2目标基因。
靶点信息
化学数据
| 目录号 | A11757 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 526.67 |
| Formula | C31H38N6O2 |
| 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. | 1346574-57-9 |
| Synonyms | GSK 126, GSK-126 |
| SMILES | CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C |
溶解度
| In vitro (25°C) | DMSO | Warmed: 3 mg/mL (5.69 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+corn oil | 0.4 mg/mL |
*<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 | 18.99 mL | 94.94 mL | 189.87 mL |
| 0.5 mM | 3.8 mL | 18.99 mL | 37.97 mL |
| 1 mM | 1.9 mL | 9.49 mL | 18.99 mL |
| 5 mM | 0.38 mL | 1.9 mL | 3.8 mL |
*The above data is based on the productmolecular weight 526.67. 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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