生物活性
UNC-1999是生物可利用抑制剂，对野生型和突变型ezh2以及ezh1具有高体外效力，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。
靶点信息
| EZH2 (Cell-free assay) | EZH1 (Cell-free assay) | | | |
| 2 nM | 45 nM | | | |
化学数据
| 目录号 | A13166 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 569.74 |
| Formula | C33H43N7O2 |
| 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. | 1431612-23-5 |
| Synonyms | UNC 1999, UNC1999 |
| SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C |
溶解度
| In vitro | DMSO | 17 mg/mL (29.84 mM) |
| Water | Insoluble |
| Ethanol | 43 mg/mL (75.47 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 | 17.55 mL | 87.76 mL | 175.52 mL |
| 0.5 mM | 3.51 mL | 17.55 mL | 35.1 mL |
| 1 mM | 1.76 mL | 8.78 mL | 17.55 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.51 mL |
*The above data is based on the productmolecular weight 569.74. 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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