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Staurosporine (CGP 41251)

potent, cell permeable PKC inhibitor

Staurosporine (CGP 41251)

Catalog No. A8192
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
1mg $50.00 In stock
5mg $200.00 In stock
10mg $350.00 In stock

All inclusive: Shipping and all other fees included

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Bozza, William P., et al. "The Use of a Stably Expressed FRET Biosensor for Determining the Potency of Cancer Drugs." PloS one 9.9 (2014): e107010. PMID:25188024

Quality Control

Quality Control & MSDS

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Chemical structure

Staurosporine(CGP 41251)

Related Biological Data

Staurosporine(CGP 41251)

Related Biological Data

Staurosporine(CGP 41251)

Related Biological Data

Staurosporine(CGP 41251)

Biological Activity

Description Staurosporine is a potent inhibitor of PKC for PKCα, PKCγ and PKCη with IC50 values of 2 nM, 5 nM and 4 nM,respectively.
Targets PKCα PKCγ PKCη PKCδ PKCε PKCζ
IC50 2 nM 5 nM 4 nM 20 nM 73 nM 1086 nM

Protocol

Cell experiment:

Cell lines

A31 cell lines, CHO-KDR cell lines, Mo-7e cell lines and A431 cell lines.

Preparation method

This product is soluble in DMSO mostly at 199 mM. It is also soluble in water with no more than 1 mM.

Reacting condition

24 h; IC50=0.08 mM (A31 cell lines), IC50=0.30 mM (Mo-7e cell lines), IC50=1.0 mM (CHO-KDR cell lines).

Applications

CGP 41251 inhibited the ligand-induced autophosphorylation of the receptors for platelet-derived growth factor (PDGF) (IC50=0.08 mM) in A31 cell lines, stem cell factor (c-Kit, IC50=0.30 mM) in Mo-7e cell lines, and for VEGF (KDR, IC50=1.0 mM) in CHO-KDR cell lines, but did not affect the ligand-induced autophosphorylation of the receptors for insulin, IGF-I, or epidermal growth factor (EGF) in A431 cell lines.

Animal experiment:

Animal models

Athymic nude mice

Dosage form

75 mg/kg/day; oral taken.

Application

The treatment with CGP 41251 (75 mg/kg/day p.o.) completely inhibits the angiogenic response to VEGF, but not to bFGF. Thus, CGP41251 may suppress tumor growth by inhibiting tumor angiogenesis (via its effects on the VEGF-R tyrosine kinases) in addition to directly inhibiting tumor cell proliferation (via its effects on PKCs). This anti-angiogenic action may contribute to the antimetastatic and broad antitumor activity displayed by CGP 41251, as well as the synergy with cytotoxic agents.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Andrejauskas-Buchdunger E, Regenass U. Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251[J]. Cancer research, 1992, 52(19): 5353-5358.

[2] Fabbro D, Buchdunger E, Wood J, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent[J]. Pharmacology & therapeutics, 1999, 82(2): 293-301.

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Chemical Properties

Cas No. 62996-74-1 SDF Download SDF
Synonyms CGP41251, CGP-41251,Staurosporine
Chemical Name (5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14(5H)-one
Canonical 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
Formula C28H26N4O3 M.Wt 466.53
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Background

Staurosporine, an alkaloid produced in Streptomyces staurospores originally as an antifungal agent, is an inhibitor of a broad spectrum of protein kinases, including protein kinase C (PKC), Camp-dependent protein kinase (PKA), phosphorylase kinase, ribosomal protein S6 kinase, epidermal growth factor receptor (EGF-R) kinase and Ca2+/calmodulin-dependent protein kinase II (Ca/CaM PKII). The inhibition potency is strongest for PKC (IC50 = 2.7 nM) but several-fold lower for other protein kinases. Staurosporine exhibits a strong cytotoxicity to some mammalian tumor cell lines, induces cell apoptosis, and arrests fission yeast cell elongation specifically at a stage immediately after cell division.

Reference

Takashi Toda, Mizuki Shimanuki, and Mitsuhiro Yanagida. Fission yeast genes that confer resistance to staurosporine encode an AP-1-like transcription factor and a protein kinase related to the mammalian ERK1/MAP2 and budding yeast FUS3 and KSS1 kinases. Genes Dev. 1991 5: 60-73

Michelle M. Hill, Mirjana Andelkovic, Derek P. Brazil, Stefano Ferrari, Doriano Fabbro, and Brian A. Hemmings. Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a Staurosporine-insensitive kinase. J. Biol. Chem 2001, 276: 25643-25646.

Flavio Meggio, Arianna Donella Deana, Maria Ruzzene, Anna M. Brunati, Luca Cesaro, Barbara Guerra, Thomas Meyer, Helmut Mett, Doriano Fabbro, Pascal Furet, Grazyna Dobrowolska, and Lorenzo A. Pinna. Different susceptibility of protein kinases to staurosporine inhibition kinetic studies and molecular bases for the resistance of protein kinase CK2. Eur. J. Biochem. 234, 317-322 (1995)