A cell-permeable PKC inhibitor
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K252c

Item No. 13514

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one
CAS Number
85753-43-1
Synonyms
  • SD 1825
  • Staurosporine aglycone
Molecular Formula
C20H13N3O
Formula Weight
311.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 500 µg/mlDMSO: 25 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: slightly soluble
λmax
233, 290, 333, 359 nm
SMILES
O=C1NCC2=C1C(C3=CC=CC=C3N4)=C4C5=C2C6=C(C=CC=C6)N5
InChi Code
InChI=1S/C20H13N3O/c24-20-17-12(9-21-20)15-10-5-1-3-7-13(10)22-18(15)19-16(17)11-6-2-4-8-14(11)23-19/h1-8,22-23H,9H2,(H,21,24)
InChi Key
MEXUTNIFSHFQRG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $96

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    5 mg

    $376

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    10 mg

    $655

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    Product Description

    K252c is a cell-permeable PKC inhibitor (IC50s = 2.45 and 25.7 µM for PKC and PKA, respectively).1 It induces apoptosis in human chronic myelogenous leukemia cancer cells.2 In human foreskin fibroblast cells, it reduces focus formation induced by human cytomegalovirus (HCMV) strains sensitive and resistant to Ganciclovir (Item No. 13853) with IC50s of 0.32 and 0.17 µM for HCMV A6245 and HCMV-6, respectively.3 It also inhibits the non-kinase enzymes β-lactamase, chymotrypsin, and malate dehydrogenase with IC50s of 8, 10, and 8 µM, suggesting less kinase-selectivity than was originally described.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pereira, E.R., Belin, L., Sancelme, M., et al. Structure-activity relationships in a series of substituted indolocarbazoles: Topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. J. Med. Chem. 39(22), 4471-4477 (1996).

    2. Liu, R., Zhu, T., Li, D., et al. Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z2039-2. Arch. Pharm. Res. 30(3), 270-274 (2007).

    3. Zimmermann, A., Wilts, H., Lenhardt, M., et al. Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase. Antiviral Res. 48(1), 49-60 (2000).

    4. McGovern, S.L., and Shoichet, B.K. Kinase inhibitors: Not just for kinases anymore. J. Med. Chem. 46(8), 1478-1483 (2003).