A potent inhibitor of protein kinase C
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Staurosporine

Item No. 81590

Technical Information
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
Synonyms
  • Stsp
Molecular Formula
C28H26N4O3
Formula Weight
Purity
≥98%
A solid
DMSO: 500 µg/mlMethanol: 2 mg/ml
λmax
241, 295, 337, 355, 373 nm
SMILES
[H][C@]12N(C3=C(N([C@](O2)(C)[C@H](OC)[C@H](NC)C1)C4=C5C=CC=C4)C5=C(CNC6=O)C6=C37)C8=C7C=CC=C8
InChi Code
InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
InChi Key
HKSZLNNOFSGOKW-FYTWVXJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

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

    2. McGlynn, E., Liβz, J., Reutener, S., et alExpression 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, 427-435 (1999).

    Product Citations

    Lee, K.P., Elster, S., Epstein, B., et alPD-1 protects expanding human T cells from premature restimulation-induced cell death by modulating TCR and CD28 signaling. Cell Death Dis. 17(1), 272 (2026).

    Nakamura, T., Hipp, C., Mourão, A.S.D., et alPhase separation of FSP1 promotes ferroptosis. Nature 619, 371-377 (2023).

    Liu, X., Nie, L., Zhang, Y., et alActin cytoskeleton vulnerability to disulfide stress mediates disulfidptosis. Nat. Cell. Biol. 25(3), 404-414 (2023).

    Njomen, E., Vanecek, A., Lansdell, T.A., et alSmall molecule 20S proteasome enhancer regulates MYC protein stability and exhibits antitumor activity in multiple myeloma. Biomedicines 10(5), 938 (2022).

    Mishima, E., Ito, J., Wu, Z., et alA non-canonical vitamin K cycle is a potent ferroptosis suppressor. Nature 608(7924), 778-783 (2022).

    Alavi, M.V. Tau phosphorylation and OPA1 proteolysis are unrelated events: Implications for Alzheimer’s Disease. Biochim. Biophys. Acta Mol. Cell Res. 1868(12), 119116 (2021).

    Rana, P.S., Gibbons, B.A., Vereninov, A.A., et alCalibration and characterization of intracellular Asante Potassium Green probes, APG-2 and APG-4. Anal. Biochem. 567, 8-13 (2019).

    Bosnakovski, D., Choi, S.H., Strasser, J.M., et alHigh-throughput screening identifies inhibitors of DUX4-induced myoblast toxicity. Skelet. Muscle 4(4), (2014).

    Ayers, S., Graf, T.N., Adcock, A.F., et alResorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).