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Staurosporine

Apoptosis inducer. Protein kinase inhibitor.
 
ALX-380-014-C100 100 µg 45.00 USD
 
ALX-380-014-C250 250 µg 95.00 USD
 
ALX-380-014-M001 1 mg 275.00 USD
 
ALX-380-014-M005 5 mg 1,200.00 USD
 
Replaces Prod. #: BML-EI156

Model apoptosis inducer. Potent cell-permeable inhibitor of a variety of protein kinases, e.g. protein kinase C (PKC), CDK1/cyclin B (IC50~5nM), CDK2/cyclin A (IC50=7nM), CDK4/cyclin D (IC50=3-10µM), CDK5/p25 (IC50=4nM), GSK-3β (IC50=15nM), Pim-1 kinase (IC50=10nM).Binds do the ATP binding domain. Did not inhibit PKC-ζ. At 1µM induced apoptosis in CHO cells. Inhibits topoisomerase II directly by blocking transfer of phosphodiester bonds from DNA to active site tyrosine.

Product Specification

Alternative Name:Antibiotic AM-2282
 
Formula:C28H26N4O3
 
MW:466.5
 
Source:Isolated from Streptomyces staurosporeus.
 
CAS:62996-74-1
 
MI:14: 8802
 
RTECS:KC655000
 
Purity:≥99% (HPLC)
 
Appearance:Off-white to green powder.
 
Solubility:Soluble in ethyl acetate, DMSO (25mg/ml) or dimethyl formamide (25mg/ml); only slightly soluble in chloroform and methanol. Insoluble in water.
 
Long Term Storage:+4°C
 
Use/Stability:Stable for at least 2 years after receipt when stored +4°C.
 
Handling:Protect from light and moisture.
 
Background / Technical Information:Replacement for ADI-HPK-112
 
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Product Literature References

Prolyl-4-hydroxylase domain 3 (PHD3) is a critical terminator for cell survival of macrophages under stress conditions: L. Swain, et al.; J. Leukoc. Biol. (2014), Abstract;
Curcumin attenuates staurosporine-mediated death of retinal ganglion cells: B. Burugula, et al.; Invest. Ophthalmol. Vis. Sci. 52, 4263 (2011), Abstract; Full Text
FKBP51 protects 661w cell culture from staurosporine-induced apoptosis: D.R. Daudt & T. Yorio; Mol. Vis. 17, 1172 (2011), Abstract; Full Text
Neuronal differentiation by analogs of staurosporine: A.F. Thompson & L.A. Levin; Neurochem. Int. 56, 554 (2010), Abstract; Full Text
The antiviral adaptor proteins Cardif and Trif are processed and inactivated by caspases: M. Rebsamen, et al.; Cell Death Differ. 15, 1804 (2008), Abstract;
The prevention of spontaneous apoptosis of follicular lymphoma B cells by a follicular dendritic cell line: involvement of caspase-3, caspase-8 and c-FLIP: J.J. Goval, et al.; Haematologica 93, 1169 (2008), Application(s): WB using human follicular lymphoma lysate, Abstract; Full Text
Pim-1 ligand-bound structures reveal the mechanism of serine/threonine kinase inhibition by LY294002: M.D. Jacobs, et al.; J.Biol.Chem. 280, 13728 (2005), Abstract;
Single-cell fluorescence resonance energy transfer analysis demonstrates that caspase activation during apoptosis is a rapid process. Role of caspase-3: M. Rehm, et al.; J. Biol. Chem. 277, 24506 (2002), Abstract; Full Text
Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a staurosporine-insensitive kinase: M.M. Hill, et al.; J. Biol. Chem. 276, 25643 (2001), Abstract; Full Text
Caspase-8 activation and bid cleavage contribute to MCF7 cellular execution in a caspase-3-dependent manner during staurosporine-mediated apoptosis: D. Tang, et al.; J. Biol. Chem. 275, 9303 (2000), Abstract; Full Text
Changes in mitochondrial membrane potential during staurosporine- induced apoptosis in Jurkat cells: J.L. Scarlett, et al.; FEBS Lett. 475, 267 (2000), Abstract;
Dissociation of staurosporine-induced apoptosis from G2-M arrest in SW620 human colonic carcinoma cells: initiation of the apoptotic cascade is associated with elevation of the mitochondrial membrane potential (deltapsim): B.G. Heerdt, et al.; Cancer Res. 60, 6704 (2000), Abstract;
Equivalent death of P-glycoprotein expressing and nonexpressing cells induced by the protein kinase C inhibitor staurosporine: K.M. Tainton, et al.; BBRC 276, 231 (2000), Abstract;
Glycogen synthase kinase-3beta facilitates staurosporine- and heat shock-induced apoptosis. Protection by lithium: G.N. Bijur, et al.; J. Biol. Chem. 275, 7583 (2000), Abstract; Full Text
Molecular mechanism of staurosporine-induced apoptosis in osteoblasts: H.J. Chae, et al.; Pharmacol. Res. 42, 373 (2000), Abstract;
Caspase-3-dependent cleavage of Bcl-2 promotes release of cytochrome c: D.G. Kirsch, et al.; J. Biol. Chem. 274, 21155 (1999), Abstract; Full Text
Characterization of the cell death process induced by staurosporine in human neuroblastoma cell lines: J. Boix, et al.; Neuropharmacology 36, 811 (1997), Abstract;
Cleavage of sterol regulatory element binding proteins (SREBPs) by CPP32 during apoptosis: X. Wang et al.; Embo J. 15, 1012 (1996), Abstract;
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review, Abstract;
Mechanism of topoisomerase II inhibition by staurosporine and other protein kinase inhibitors: P. Lassota et al.; J. Biol. Chem. 271, 26418 (1996), Abstract;
Staurosporine and ent-staurosporine: the first total synthesis, prospects for a regioselective approach, and activity profile: J.T. Link et al.; J. Am. Chem. Soc. 118, 2825 (1996),
Staurosporine induces programmed cell death in embryonic neurons and activation of the ceramide pathway: D.A. Wiesner & G. Dawson; J. Neurochem 66, 1418 (1996), Abstract;
First total synthesis of Staurosporine and ent-Staurosporine: J.T. Link et al.; J. Am. Chem. Soc. 117, 552 (1995),
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue: C.M Seynaeve et al.; Mol. Pharmacol. 45, 1207 (1994), Abstract;
Induction of a common pathway of apoptosis by staurosporine: R. Bertrand, et al.; Exp. Cell Res. 211, 314 (1994), Abstract;
Is staurosporine a specific inhibitor of protein kinase C in intact porcine coronary arteries?: M. Kageyama, et al.; J. Pharmacol. Exp. Ther. 259, 1019 (1991), Abstract;
Staurosporine: an effective inhibitor for Ca2+/calmodulin-dependent protein kinase II: N. Yanagihara, et al.; J. Neurochem. 56, 294 (1991), Abstract;
Staurosporine, a protein kinase C inhibitor interferes with proliferation of arterial smooth muscle cells: H. Matsumoto & Y. Sasaki; Biochem. Biophys. Res. Commun. 158, 105 (1989), Abstract;
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review), Abstract;
Contrasting actions of staurosporine, a protein kinase C inhibitor, on human neutrophils and primary mouse epidermal cells: T. Sako, et al.; Cancer Res. 48, 4646 (1988), Abstract;
Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60: N. Nakano, et al.; J. Antibiot. (Tokyo) 40, 706 (1987), Abstract;
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase: T. Tamaoki, et al.; BBRC 135, 397 (1986), Abstract;
Staurosporine, a potent platelet aggregation inhibitor from a Streptomyces species: S. Oka, et al.; Agric. Biol. Chem. 50, 2723 (1986),
A. Furusaki, et al.; J. C. S. Chem. Commun. 800 (1978),
A new alkaloid AM-2282 of Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization: S. Omura, et al.; J. Antibiot. (Tokyo) 30, 275 (1977), Abstract;

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