[CAS NO. 62996-74-1] Staurosporine

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PRODUCTS SPECIFICATIONS [62996-74-1]

Catalog

HY-15141

Brand

MCE

CAS

62996-74-1

DESCRIPTION [62996-74-1]

Overview

MDL	-
Molecular Weight	466.53
Molecular Formula	C28H26N4O3
SMILES	O=C(NC1)C2=C1C3=C(C4=C2C5=C(C=CC=C5)N4[C@H]6C[C@@H](NC)[C@@H](OC)[C@]7(C)O6)N7C8=CC=CC=C83

For research use only. We do not sell to patients.

64 Publications Citing Use of MCE

Summary

Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC ₅₀ s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC , PKA , c-Fgr , and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC ₅₀ of 3 μM. Staurosporine is an apoptosis inducer ^[1] ^[2] ^[3] ^[4] ^[5] .

IC50 & Target

PKC

6 nM (IC ₅₀ )

PKA

15 nM (IC ₅₀ )

c-Fgr

2 nM (IC ₅₀ )

Phosphorylase kinase

3 nM (IC ₅₀ )

S6 kinase (70 kDa)

5 nM (IC ₅₀ )

v-Src

6 nM (IC ₅₀ )

cdc2

9 nM (IC ₅₀ )

TPK-IIB/Syk

16 nM (IC ₅₀ )

Ca ²⁺ /CaM PK-I1

20 nM (IC ₅₀ )

MLCK

21 nM (IC ₅₀ )

IR

61 nM (IC ₅₀ )

EGF-R

100 nM (IC ₅₀ )

ERK-1

1500 nM (IC ₅₀ )

CSK

2000 nM (IC ₅₀ )

IGF-IR

6150 nM (IC ₅₀ )

CK2

19500 nM (IC ₅₀ )

CK1

163500 nM (IC ₅₀ )

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Source

Streptomyces staurosporeus

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL ( 133.97 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 0.5% CMC-Na /saline water

Solubility: 3.33 mg/mL (7.14 mM); Suspension solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (4.46 mM); Suspended solution; Need ultrasonic
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3′,2′,1′-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-11-(methylamino)-, (9S,10R,11R,13R)-

9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3′,2′,1′-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-11-(methylamino)-, [9S-(9α,10β,11β,13α)]-

(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3′,2′,1′-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one

Antibiotic AM 2282

Staurosporine

Staurosporin

AM-2282

Alkaloid AM-2282 from Streptomyces

(+)-Staurosporine

Antibiotic 230

CGP 39360