Staurosporine


Catalog No. size PriceQuantity
M6779-2 2mg solid $147
M6779-10 10mg solid $596

Description

Cas:62996-74-1

Product Information

Staurosporine, also known as antibiotic AM-2282 or STS, is a potent, non-selective inhibitor of protein kinases, including protein kinase C with promising anti-cancer activity. 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. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity.

 

Chemical Formula:C28H26N4O3

 

Exact Mass: 466.20049

 

Molecular Weight: 466.54

 

Elemental Analysis: C, 72.09; H, 5.62; N, 12.01; O, 10.29

 

Synonym: 

 

AM-2282

AM2282

AM 2282

STS

Antibiotic 230

CGP 41251

CGP41251

CGP-41251

CCRIS 3272

Staurosporine

Staurosporin.

 

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

 

InChi Key:

HKSZLNNOFSGOKW-FYTWVXJKSA-N

 

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

 

SmilesCode:

CO[C@@H]1[C@@H](C[C@@H]2N3C4=C(N(C5=CC=CC=C56)[C@@]1(C)O2)C6=C7CNC(C7=C4C8=CC=CC=C83)=O)NC

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

Staurosporine, widely used as a protein kinase C (PKC) inhibitor with a broad spectrum of activity, is an alkaloid isolated from the culture broth ofStreptomyces staurospores. MC3T3E-1 osteoblasts, expose to Staurosporine (100 nM) for 12 h, release an amount of LDH (12.4±3.1%) that is similar to that release by the control cells(10.0±2.4%), indicating the relative absence of lytic death, which occurs in necrosis. In addition, treatment with Staurosporine (100 nM) results in morphological changes, characteristic of apoptosis: a brightblue fluorescent condensed nuclei seen through a fluorescence microscope after Hoechst 33258-staining, and a reduction of cell volume.

 

In Vivo:

The inhibitory effect of Staurosporine is statistically significant at around Wk 10 of tumor promotion. Although statistically significant inhibition is not obtained with 10 ng of Staurosporine in later weeks of the experiment, a decreasing tendency in the percentages of tumor bearing mice and in average numbers of tumors per mouse is apparent. Thus, Staurosporine slightly inhibits tumor promotion of Teleocidin, even at the dose at which Staurosporine itself induced tumors. Staurosponne (0.05 and 0.1 mg/kg intraperitoneal) attenuates the impaired perlormance of water maze and passive avoidance tasks, even though the drug administration began 2 weeks after the lesion. Moreover, Staurosporine (0.1 mg/kg) partially reversed the decrease of choline acetyltransferase activity in the fronto-parietal cortex induced by basal forebrain-lesion. These results suggest that Staurosporine attenuates impairment of learning through reversal of damage to cholinergic neurons induced by basal forebrain-lesion.

 

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.

 

Products are for research use only. Not for human use.

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