Staurosporine

Modify Date: 2024-01-04 10:05:54

Staurosporine Structure
Staurosporine structure
 Common Name Staurosporine
CAS Number 62996-74-1 Molecular Weight 466.531
Density 1.6±0.1 g/cm3 Boiling Point 677.5±55.0 °C at 760 mmHg
Molecular Formula C28H26N4O3 Melting Point 270ºC
MSDS USA Flash Point 363.6±31.5 °C
Symbol GHS08
GHS08		 Signal Word Danger

 Use of Staurosporine


Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively.

 Names

Name staurosporine
Synonym More Synonyms

 Staurosporine Biological Activity

Description Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively.
Related Catalog
Target

PKC:6 nM (IC50)

c-Fgr:2 nM (IC50)

Phosphorylase kinase:3 nM (IC50)

v-Src:6 nM (IC50)

cdc2:9 nM (IC50)

TPK-IIB/Syk:16 nM (IC50)

Ca2+/CaM PK-I1:20 nM (IC50)

MLCK:21 nM (IC50)

IR:61 nM (IC50)

EGF-R:100 nM (IC50)

ERK-1:1500 nM (IC50)

CSK:2000 nM (IC50)

IGF-IR:6150 nM (IC50)

CK2:19500 nM (IC50)

CK1:163500 nM (IC50)

S6 kinase (70 kDa):5 nM (IC50)

PKA:15 nM (IC50)
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 of Streptomyces 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[2].
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[3]. 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[4].
Kinase Assay MC3T3E-1 cells (2×106 cells/group) are treated with 100 nM Staurosporine for various time periods and lysed in a lysis buffer (EB buffer: 1% Triton X-100, 10 mM Tris, pH 7.6, 50 mM NaCl, 1 mg/mL Aprotinin, 5 mM EDTA, 50 mM NaF, 0.1% 2-mercaptoethanol, and 100 μM sodium orthovanadate). The lysate of the cells is subjected to centrifugation at 12 000 g at 4°C for 30 min. Soluble fraction is collected and incubated with anti-JNK1 antibodies. After incubation on ice for 3 h, 100 μL of a 10% solution of formalin-fixed Staphylococcus aureus is added to the anti-JNK1 immunoprecipitates and further incubated on ice for 1 h. The absorbed immune complex is washed twice with EB buffer and PAN buffer (10 mM PIPES buffer, pH 7.0, 1% aprotinin, 100 mM NaCl). The immunecomplex is mixed with 2 μg of GST-c-Jun NT1-79 proteins as a substrate in 30 μL of the reaction buffer containing 2 μM cold ATP, 2 mM DTT, 20 mM MgCl2, 2 μCi [γ33-P]-ATP, and 20 mM Tris-HCl, pH 7.5 at 30°C for 20 min. The reaction is terminated by adding 15 μL of 3× SDS-PAGE sample buffer and boiling at 98°C for 5 min. The proteins are separated on 12% SDS-PAGE and transferred onto a nitrocellulose membrane via the semi-dry electrotransfer system. The membrane is immunoblotted with rabbit anti-JNK1 antibodies and horse radish peoxidaseconjugated anti-rabbit antibodies to visualize the signals measured by an enhanced chemiluminescence system. The gel is dried under a vacuum, and the phosphotransferase activity is visualized by autoradiography and quantified by a PhosphoImager analyzer[2].
Animal Admin Mice[3] Female CD-I mice are used. Various amounts of Staurosporine in 10 μL of acetone are applied to the ears of 8-wk-old CD-I mice. The extent of irritation is expressed as the minimum dose of the compound causing irritation. Induction of HOC in Mouse Skin Staurosporine in 0.1 mL of acetone is applied to the skin of the backs of CD-I mice, and a crude enzyme extract is obtained from the skin 18 h later. HDC activity is expressed as pmol of CO2 released per mg of protein per l h of incubation. Induction of ODC in Mouse Skin Staurosporine in 0.2 mL of acetone is applied to the skin of the backs of CD-I mice. After 4 h, a crude enzyme extract is prepared from the epidermis, and its ODC activity is measured. Enzyme activity is expressed as nmol of CO2 per mg of protein per 30 min of incubation. Rats[4] Male Kbl Wistar rats(weighing 270 to 310 g) are used. In the group which is given Staurosporine for 2 weeks, the water maze task and Staurosporine administration are started 2 weeks after the BF-lesion, and the passive avoidance task is carried out 4 weeks after the BFlesion. The rat received Staurosporine at doses of 0.01, 0.03, 0.1, and 0.3 mg/kg (i.p., N=10 in each group for 2 weeks) 30 mm prior to the water maze training sessions and the passive avoidance task acquisitiontrial. In the group which is given Staurosporine for 4 weeks, the drug is first given 2 weeks after the BF-lesion. The water maze task is carried out 4 weeks after the BF-lesion. The passive avoidance task is carried out 6 weeks after the BF-lesion. The rat received Staurosporine at 0.05, 0.1, and 0.2 mg/kg (i.p., N=10 in each group) once a day for 2 weeks before training, and for 2 weeks after the water maze training sessions and the passive avoidance task acquisition trial. Staurosporine is suspended in 0.3% of sodium carboxymethyl cellulose. The vehicle is administered to the non-lesioned controls and the lesioned controls on the same schedule as the Staurosporine-treated animals.
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.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 677.5±55.0 °C at 760 mmHg
Melting Point 270ºC
Molecular Formula C28H26N4O3
Molecular Weight 466.531
Flash Point 363.6±31.5 °C
Exact Mass 466.200500
PSA 69.45000
LogP 4.40
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.810

 MSDS

Name: Staurosporine Material Safety Data Sheet
Synonym: Antibiotic AM-228
CAS: 62996-74-1
Section 1 - Chemical Product MSDS Name:Staurosporine Material Safety Data Sheet
Synonym:Antibiotic AM-228
Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS
CAS# Chemical Name content EINECS#
62996-74-1 Staurosporine ca 100 unlisted
Hazard Symbols: XN
Risk Phrases: 40
Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
Limited evidence of a carcinogenic effect.Light sensitive.Moisture sensitive.The toxicological properties of this material have not been fully investigated.
Potential Health Effects
Eye:
May cause eye irritation.
Skin:
May cause skin irritation.
Ingestion:
May cause irritation of the digestive tract. The toxicological properties of this substance have not been fully investigated.
Inhalation:
May cause respiratory tract irritation. The toxicological properties of this substance have not been fully investigated.
Chronic:
No information found.
Section 4 - FIRST AID MEASURES
Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid.
Skin:
Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes. Wash clothing before reuse.
Ingestion:
Never give anything by mouth to an unconscious person. Get medical aid. Do NOT induce vomiting. If conscious and alert, rinse mouth and drink 2-4 cupfuls of milk or water. Wash mouth out with water.
Inhalation:
Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid.
Notes to Physician:
Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion.
Non-combustible, substance itself does not burn but may decompose upon heating to produce irritating, corrosive and/or toxic fumes.
Extinguishing Media:
Substance is noncombustible; use agent most appropriate to extinguish surrounding fire. Do NOT get water inside containers. Use water spray, dry chemical, carbon dioxide, or appropriate foam.
Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Vacuum or sweep up material and place into a suitable disposal container. Clean up spills immediately, observing precautions in the Protective Equipment section. Avoid generating dusty conditions.
Provide ventilation. Do not get water inside containers.
Section 7 - HANDLING and STORAGE
Handling:
Wash thoroughly after handling. Use with adequate ventilation.
Minimize dust generation and accumulation. Avoid contact with eyes, skin, and clothing. Keep container tightly closed. Avoid ingestion and inhalation. Store protected from light. Do not allow contact with water. Keep from contact with moist air and steam.
Storage:
Do not store in direct sunlight. Store in a tightly closed container. Store in a cool, dry, well-ventilated area away from incompatible substances. Keep refrigerated. (Store below 4C/39F.) Store protected from moisture. Store protected from light.
Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use adequate ventilation to keep airborne concentrations low.
Exposure Limits CAS# 62996-74-1: Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear appropriate protective clothing to prevent skin exposure.
Respirators:
A respiratory protection program that meets OSHA's 29 CFR 1910.134 and ANSI Z88.2 requirements or European Standard EN 149 must be followed whenever workplace conditions warrant respirator use.
Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Powder
Color: off-white
Odor: none reported
pH: Not available.
Vapor Pressure: Not available.
Viscosity: Not available.
Boiling Point: Not available.
Freezing/Melting Point: 270 deg C
Autoignition Temperature: Not applicable.
Flash Point: Not applicable.
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature:
Solubility in water:
Specific Gravity/Density:
Molecular Formula: C28H26N4O3
Molecular Weight: 466.207
Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Stable at room temperature in closed containers under normal storage and handling conditions.
Conditions to Avoid:
Incompatible materials, light, moisture, excess heat, exposure to moist air or water.
Incompatibilities with Other Materials:
Moisture, strong oxidizing agents.
Hazardous Decomposition Products:
Hydrogen chloride, nitrogen oxides, carbon monoxide, irritating and toxic fumes and gases, carbon dioxide.
Hazardous Polymerization: Will not occur.
Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 62996-74-1: KC6550000 LD50/LC50:
Not available.
Carcinogenicity:
Staurosporine - Not listed by ACGIH, IARC, or NTP.
Other:
See actual entry in RTECS for complete information.
Section 12 - ECOLOGICAL INFORMATION

Section 13 - DISPOSAL CONSIDERATIONS
Dispose of in a manner consistent with federal, state, and local regulations.
Section 14 - TRANSPORT INFORMATION

IATA
No information available.
IMO
No information available.
RID/ADR
No information available.
Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: XN
Risk Phrases:
R 40 Limited evidence of a carcinogenic effect.
Safety Phrases:
S 28A After contact with skin, wash immediately with
plenty of water.
S 36/37 Wear suitable protective clothing and
gloves.
S 37 Wear suitable gloves.
S 45 In case of accident or if you feel unwell, seek
medical advice immediately (show the label where
possible).
WGK (Water Danger/Protection)
CAS# 62996-74-1: No information available.
Canada
None of the chemicals in this product are listed on the DSL/NDSL list.
CAS# 62996-74-1 is not listed on Canada's Ingredient Disclosure List.
US FEDERAL
TSCA
CAS# 62996-74-1 is not listed on the TSCA inventory.
It is for research and development use only.

SECTION 16 - ADDITIONAL INFORMATION
N/A

 Safety Information

Symbol GHS08
GHS08
Signal Word Danger
Hazard Statements H340-H350
Precautionary Statements P201-P280-P308 + P313
Personal Protective Equipment Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
Hazard Codes Xn;T;Xi
Risk Phrases R40
Safety Phrases S53-S36-S37
RIDADR UN 2811 6.1 / PGII
WGK Germany 2
RTECS KC6550000
HS Code 29419090

 Precursor & DownStream

Precursor  2

DownStream  0

 Articles209

More Articles
TAp73 promotes cell survival upon genotoxic stress by inhibiting p53 activity.

Oncotarget 5(18) , 8107-22, (2014)

p53 plays a key role in regulating DNA damage response by suppressing cell cycle progression or inducing apoptosis depending on extent of DNA damage. However, it is not clear why mild genotoxic stress...
Unmethylated CpG motifs in the L. donovani DNA regulate TLR9-dependent delay of programmed cell death in macrophages.

J. Leukoc. Biol. 97(2) , 363-78, (2015)

Regulation of macrophage PCD plays an important role in pathogenesis of leishmaniasis. However, the precise involvement of any parasite molecule in this process remains uncertain. In the current study...
Higher vulnerability and stress sensitivity of neuronal precursor cells carrying an alpha-synuclein gene triplication.

PLoS ONE 9(11) , e112413, (2014)

Parkinson disease (PD) is a multi-factorial neurodegenerative disorder with loss of dopaminergic neurons in the substantia nigra and characteristic intracellular inclusions, called Lewy bodies. Geneti...

 Synonyms

Stauroporine
6,10-Epoxy-6H,16H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-16-one, 7,8,9,10,17,18-hexahydro-7-methoxy-6-methyl-8-(methylamino)-, (6S,7R,8R,10R)-
(2S,3R,4R,6R)-3-Methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1.0.0.0.0.0]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one
Staurosporine
staurosphorine
ANTIBIOTIC M 193
MFCD00077402
Antibiotic 230
antibiotic am 2282
ANTIBIOTIC AM-2282
AM-2282
STSP
Staurosporin
Top Suppliers:I want be here

Get all suppliers and price by the below link:

Staurosporine suppliers

Price: $135/10mM*1mLinDMSO

Reference only. check more Staurosporine price

Related Compounds: More...
(-)-Staurosporine
160335-45-5
staurosporine
622996-74-1
5'-Hydroxy-staurosporine
308847-74-7
7-oxo Staurosporine
125035-83-8
1,1',2,2',3,3',4,4'-Octahydro Staurosporine
220038-18-6
6-N-((benzyloxy)methyl)-ent-7-oxo-4'-N-(tert-butyloxycarbonyl)staurosporine
174148-74-4
1,2,3,4-Tetrahydrostaurosporine
220038-19-7
STAUROSPORINE AGLYCON
118458-54-1
staurosporine aglycon
85753-43-1
Chemsrc provides Staurosporine(CAS#:62996-74-1) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Staurosporine are included as well.>> amp version: Staurosporine

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved