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Purity: ≥98%
Staurosporine (formerly also known as antibiotic AM-2282; CCRIS 3272; CGP 41251 or STS) is a naturally occuring, potent and non-selective PKC inhibitor with anti-fungal to anti-hypertensive effects. It inhibits PKCα, PKCγ and PKCη with IC50s of 2 nM, 5 nM and 4 nM, respectively. Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. It less potent to PKCδ (20 nM), PKCε (73 nM) and has little active to PKCζ (1086 nM) in cell-free assays. It also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus with anti-fungal to anti-hypertensive effects.
| ln Vitro |
Staurosporine is an alkaloid with broad-spectrum activity that is frequently utilized as a protein kinase C (PKC) inhibitor. It may be extracted from the culture media of Streptomyces staurospores. After being treated to staurosporine (100 nM) for 12 hours, MC3T3E-1 osteoblasts released LDH (12.4±3.1%) in proportions comparable to control cells (10.0±2.4%), suggesting a relative absence of lytic cell death that takes place during necrosis. Moreover, Staurosporine (100 nM) treatment causes morphological alterations that are indicative of apoptosis: fluorescence microscopy reveals vivid blue luminous concentrated nuclei and a reduction in cell volume following Hoechst 33258 staining [2].
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| ln Vivo |
About the tenth week of tumor promotion, staurosporine's inhibitory impact started to show statistical significance. Despite the lack of a statistically significant inhibitory effect with 10 ng Staurosporine in the later weeks of the experiment, the average number of tumors per mouse and the percentage of tumor-bearing mice showed a definite decreasing trend. Thus, even at levels where Staurosporine alone would cause tumors, Staurosporine somewhat reduces the tumor-promoting effects of Teleocidin [3]. Even when administered two weeks after the injury, staurosponne (0.05 and 0.1 mg/kg intraperitoneally) reduced poor performance on the water maze and passive avoidance tests. Moreover, the reduction in choline acetyltransferase activity in the frontoparietal cortex brought on by basal forebrain injuries was largely restored by staurosporine (0.1 mg/kg). According to these findings, staurosporine may help learning disabled people by repairing the cholinergic neurons that have been harmed by basal forebrain injury [4].
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| References |
[1]. Meggio F, et al. Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. Eur J Biochem. 1995 Nov 15;234(1):317-22.
[2]. Chae HJ, et al. Molecular mechanism of staurosporine-induced apoptosis in osteoblasts. Pharmacol Res. 2000 Oct;42(4):373-81. [3]. Yoshizawa S, et al. Tumor-promoting activity of staurosporine, a protein kinase inhibitor on mouse skin.Cancer Res. 1990 Aug 15;50(16):4974-8. [4]. Nabeshima T, et al. Staurosporine facilitates recovery from the basal forebrain-lesion-induced impairment of learning and deficit of cholinergic neuron in rats. J Pharmacol Exp Ther. 1991 May;257(2):562-6. [5]. Yujie Ren, et al. The ORF3a Protein of SARS-CoV-2 Induces Apoptosis in Cells. Cell Mol Immunol. 2020 Jun 18;1-3 |
| Molecular Formula |
C28H26N4O3
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| Molecular Weight |
466.53
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| CAS # |
62996-74-1
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| SMILES |
O1C2([H])C([H])([H])C([H])(C([H])([C@@]1(C([H])([H])[H])N1C3=C([H])C([H])=C([H])C([H])=C3C3=C4C([H])([H])N([H])C(C4=C4C5=C([H])C([H])=C([H])C([H])=C5N2C4=C13)=O)OC([H])([H])[H])N([H])C([H])([H])[H]
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| InChi Key |
HKSZLNNOFSGOKW-FYTWVXJKSA-N
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| InChi Code |
InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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| Chemical Name |
(5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14-one
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1435 mL | 10.7174 mL | 21.4348 mL | |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.2870 mL | |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1435 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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