生物活性
Indirubin是中国抗白血病药物的活性成分,是一种有效的细胞周期蛋白依赖性激酶和GSK-3β抑制剂,IC50约为5 μM和0.6 μM。
Targets
| Target | Value |
| GSK-3β | IC50: 0.6μM |
| CDK2/CyclinA | IC50: 2.2μM |
| CDK5/p35 | IC50: 5.5μM |
| CDK1/CyclinB | IC50: 10μM |
| C-Raf | IC50: >10μM |
| CDK4/CyclinD1 | IC50: 12μM |
| c-Src | IC50: 18μM |
| ERK2 | IC50: 43μM |
| ERK1 | IC50: >100μM |
| MAPKK | IC50: >100μM |
| PKCα | IC50: >100μM |
| PKCβ1 | IC50: >100μM |
| PKCβ2 | IC50: >100μM |
| PKCγ | IC50: >100μM |
| PKCδ | IC50: >100μM |
| PKCε | IC50: >100μM |
| PKCη | IC50: >100μM |
| PKCζ | IC50: >100μM |
| c-Abl | IC50: >1000μM |
化学数据
| 目录号 | A10471 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 262.3 |
| Formula | C16H10N2O2 |
| 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. | 479-41-4 |
| Synonyms | Couroupitine B, Indigo red |
| SMILES | C1=CC=C2C(=C1)/C(=C\3/C(=O)C4=CC=CC=C4N3)/C(=O)N2 |
溶解度
| In vitro | DMSO | 48 mg/mL (183.02 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<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 | 38.12 mL | 190.62 mL | 381.24 mL |
| 0.5 mM | 7.62 mL | 38.12 mL | 76.25 mL |
| 1 mM | 3.81 mL | 19.06 mL | 38.12 mL |
| 5 mM | 0.76 mL | 3.81 mL | 7.62 mL |
*The above data is based on the productmolecular weight 262.3 . 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.