生物活性
Staurosporine是一种天然产物，最初于1977年从Streptomyces staurosporeus细菌中分离出来。星形孢菌素的主要生物学活性是通过防止ATP与激酶的结合来抑制蛋白激酶。是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。
Targets
| Target | Value |
| PKCα | IC50: 2nM |
| c-Fgr | IC50: 2nM |
| phosphorylasekinase | IC50: 3nM |
| PKCη | IC50: 4nM |
| PKCγ | IC50: 5nM |
| S6kinase | IC50: 5nM |
| v-Src | IC50: 6nM |
| Cdc2 | IC50: 9nM |
| Cdc2 | IC50: 9nM |
| PKA | IC50: 15nM |
| Syk | IC50: 16nM |
| PKG | IC50: 18nM |
| PKCδ | IC50: 20nM |
| CaMKII | IC50: 20nM |
| Lyn | IC50: 20nM |
| MLCK | IC50: 21nM |
| PKCε | IC50: 73nM |
| PKCζ | IC50: 1086nM |
化学数据
| 目录号 | A10864 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 466.5 |
| Formula | C28H26N4O3 |
| 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. | 62996-74-1 |
| Synonyms | AM-2282, STS |
| SMILES | C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC |
溶解度
| In vitro | DMSO | 4 mg/mL (8.57 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 | 21.44 mL | 107.18 mL | 214.36 mL |
| 0.5 mM | 4.29 mL | 21.44 mL | 42.87 mL |
| 1 mM | 2.14 mL | 10.72 mL | 21.44 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.29 mL |
*The above data is based on the productmolecular weight 466.5 . 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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