Staurosporine

Staurosporine

Cayman Chemical Item Number 81590

Stsp (CAS 62996-74-1)

Staurosporine (CAS 62996-74-1)

Description

Staurosporine (Stsp) is potent inhibitor of protein kinase C (PKC) from rat brain, exhibiting an IC₅₀ value of 2.7 nM.¹ It inhibits rat recombinant PKC-α approximately 100- and 1,000-fold better than PKC-δ and PKC-ζ, respectively.² However, Stsp is non-selective in that it also inhibits the activity of a variety of other protein kinases, not only PKC isoforms.³ The biological effects of Stsp include cytotoxicity, relaxation of smooth muscle, and regulation of eNOS gene expression.^3,4

1 Tamaoki, T., Nomoto, H., Takahashi, I., et al. Staurosporine, a potent inhibitor of phospholipid/Ca++ dependent protein kinase. Biochem Biophys Res Commun 135 397-402 (1986).

2 McGlynn, E., Liebetanz, J., Reutener, S., et al. Expression and partial characterization of rat protein kinase C-δ and protein kinase C-ζ in insect cells using recombinant baculovirus. J Cell Biochem 49 239-250 (1992).

3 Ruegg, U.T., and Burgess, G.M. Staurosporine, K^-252 and UCN-01: Potent but nonspecific inhibitors of protein kinases. Trends Pharmacol Sci 10 218-220 (1989).

4 Li, H., and Förstermann, U. Structure-activity relationship of staurosporine analogs in regulating expression of endothelial nitric-oxide synthase gene. Mol Pharmacol 57 427-35 (1999).

Synonyms

Stsp

Formal Name

2,3,10,11,12,13-hexahydro-10R-methoxy-9S-methyl-11R-methylamino-9S,13R-epoxy-1H,9H-diindolo[1,2,3-gh;3’,2’,1’-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one

CAS Number

62996-74-1

Molecular Formula

C₂₈H₂₆N₄O₃

Formula Weight

466.5

Formulation

A solution in ethyl acetate

Purity

>98%

λ_max

241, 295, 337, 355, 373 nm

Stability

1 year

Storage

-20°C

Shipping

Wet ice in continental US; may vary elsewhere

SMILES

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CN[C@H]1CC2OC(C)(C1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13

Background Reading

Li, H., and Förstermann, U. Structure-activity relationship of staurosporine analogs in regulating expression of endothelial nitric-oxide synthase gene. Mol Pharmacol 57 427-35 (1999).

Tamaoki, T., Nomoto, H., Takahashi, I., et al. Staurosporine, a potent inhibitor of phospholipid/Ca++ dependent protein kinase. Biochem Biophys Res Commun 135 397-402 (1986).

Ruegg, U.T., and Burgess, G.M. Staurosporine, K^-252 and UCN-01: Potent but nonspecific inhibitors of protein kinases. Trends Pharmacol Sci 10 218-220 (1989).

McGlynn, E., Liebetanz, J., Reutener, S., et al. Expression and partial characterization of rat protein kinase C-δ and protein kinase C-ζ in insect cells using recombinant baculovirus. J Cell Biochem 49 239-250 (1992).

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Size

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1 mg 
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