Staurosporine
Catalog No. A10864
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。
- Lisa M Kim, .et al. Sustained Oncogenic Signaling in the Cytostatic State Enables Targeting of Nonproliferating Persistent Cancer Cells, Cancer Res, 2022, Sep 2;82(17):3045-3057 PMID: 35792658
- Jacobs CL, .et al. StaPLs: versatile genetically encoded modules for engineering drug-inducible proteins, Nat Methods, 2018, Jul;15(7):523-526 PMID: 29967496
- Birte Plitzko, .et al. The natural product mensacarcin induces mitochondrial toxicity and apoptosis in melanoma cells, J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
Catalog Num | A10864 |
---|---|
M. Wt | 466.5 |
Formula | C28H26N4O3 |
Purity | >98% |
Storage | at -20°C 3 years Powder |
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 |
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 |
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. |
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.