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
PKCαIC50: 2nM
c-FgrIC50: 2nM
phosphorylasekinaseIC50: 3nM
PKCηIC50: 4nM
PKCγIC50: 5nM
S6kinaseIC50: 5nM
v-SrcIC50: 6nM
Cdc2IC50: 9nM
Cdc2IC50: 9nM
PKAIC50: 15nM
SykIC50: 16nM
PKGIC50: 18nM
PKCδIC50: 20nM
CaMKIIIC50: 20nM
LynIC50: 20nM
MLCKIC50: 21nM
PKCεIC50: 73nM
PKCζIC50: 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.