生物活性
GSK 1210151A (I-BET151)是溴结构域和额外末端（BET）家族蛋白BRD2，BRD3和BRD4的新型选择性抑制剂。
靶点信息
| BRD3 (Cell-free assay) | BRD2 (Cell-free assay) | BRD4 (Cell-free assay) | | |
| 0.25 μM | 0.5 μM | 0.79 μM | | |
化学数据
| 目录号 | A11783 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 415.4 |
| Formula | C23H21N5O3 |
| 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. | 1300031-49-5 |
| Synonyms | GSK1210151A |
| SMILES | CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)[C@H](C)C5=CC=CC=N5)OC |
溶解度
| In vitro | DMSO | Insoluble |
| Water | Insoluble |
| Ethanol | 27 mg/mL (64.99 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 | 24.07 mL | 120.37 mL | 240.73 mL |
| 0.5 mM | 4.81 mL | 24.07 mL | 48.15 mL |
| 1 mM | 2.41 mL | 12.04 mL | 24.07 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.81 mL |
*The above data is based on the productmolecular weight 415.4 . 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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