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ProductsBack/K-252c [85753-43-1]
Chemical Structure
Chemical Structure
Chemical Structure

K-252c [85753-43-1]

Research Use Only
AG-CN2-0097
AdipoGen Life Sciences
CAS Number85753-43-1
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Product group Chemicals
Estimated Purity>97% (HPLC)
Molecular Weight311.4
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    K-252c [85753-43-1]
  • Delivery Days Customer
    10
  • CAS Number
    85753-43-1
  • Certification
    Research Use Only
  • Estimated Purity
    >97% (HPLC)
  • Hazard Information
    Non-hazardous
  • Molecular Formula
    C20H13N3O
  • Molecular Weight
    311.4
  • Scientific Description
    Chemical. CAS: 85753-43-1. Formula: C20H13N3O. MW: 311.4. Isolated from Streptomyces longisporoflavus. Indolocarbazole alkaloid antibiotic. Potent cell permeable reversible and ATP-competitive PKC (protein kinase C) inhibitor with 10-fold selectivity over PKA (protein kinase A). Anticancer compound. Cytotoxic againt various cancer cell lines. Apoptosis inducer. Antiviral compound against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV). LACTB (beta-lactamase), malate dehydrogenase (MDH2, MDHC, MDH1B, ME1. ME2, ME3) and chymotrypsin inhibitor. Inhibits mixed lineage kinase (MLK). - Indolocarbazole alkaloid antibiotic. [1]. Potent cell permeable reversible and ATP-competitive PKC (protein kinase C) inhibitor with 10-fold selectivity over PKA (protein kinase A) [1-5]. Anticancer compound. Cytotoxic againt various cancer cell lines [6, 9,11]. Apoptosis inducer [11]. Antiviral compound against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) [7]. LACTB (beta-lactamase), malate dehydrogenase (MDH2, MDHC, MDH1B, ME1. ME2, ME3) and chymotrypsin inhibitor [8]. Inhibits mixed lineage kinase (MLK) [10].
  • SMILES
    O=C1NCC2=C1C1=C(NC3=C1C=CC=C3)C1=C2C2=C(N1)C=CC=C2
  • Storage Instruction
    2°C to 8°C,-20°C
  • UNSPSC
    12352200

References

  • K-252b, c and d, potent inhibitors of protein kinase C from microbial origin: S. Nakanishi, et al.; J. Antibiot. 39, 1066 (1986)
  • The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. 39, 1072 (1986)
  • Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989)
  • Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds: S. Fabre, et al.; Bioorg. Med. Chem. 1, 193 (1993)
  • Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C: J. Kleinschroth, et al.; Bioorg. Med. Chem. Lett. 3, 1959 (1993)
  • Staurosporine aglycone (K252-c) and arcyriaflavin A from the marine ascidian, Eudistoma sp: P.A. Horton, et al.; Experientia 50, 843 (1994)
  • Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase: A. Zimmermann, et al.; Antiviral Res. 48, 49 (2000)
  • Kinase inhibitors: not just for kinases anymore: S.L. McGovern & B.K. Shoichet; J. Med. Chem. 46, 1478 (2003)
  • Biological targets of antitumor indolocarbazoles bearing a sugar moiety: M. Prudhomme; Curr. Med. Chem. Anticancer Agents 4, 509 (2004)
  • Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a: R.L. Hudkins, et al.; J. Med. Chem. 50, 433 (2007)