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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
| EZH2 | ||||
| 9.9 nM |
| 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. |
|||
| 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.
| 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. |
| 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 |
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