Molecular structure of K252c, CAS Number: 85753-43-1
K252c (CAS 85753-43-1)
See product citations (3)
Alternate Names:
Staurosporine Aglycone
Application:
K252c is a PKC inhibitor with selective for PKCA
CAS Number:
85753-43-1
Purity:
95%
Molecular Weight:
311.4
Molecular Formula:
C20H13N3O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
K252c is an aglycone, indolocarbazole alkaloid which is a protein kinase inhibitor of the Staurosporine family. K252c is a cell-permeable inhibitor of PKC (protein kinase C) (IC50 = 2.45 muM) that displays approximately 10-fold selectivity over PKA (protein kinase A) (IC50 = 25.7 muM). K252c is cytotoxic for A549 and P388 cells (IC50 = 2-3 mM). K252c also inhibits LACTB (beta-lactamase), malate dehydrogenase (MDH2, MDHC, MDH1B) and chymotrypsin (IC50 values are 8, 8 and 10 muM respectively). K252c displays antiviral activity against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) (IC50 values range from 0.13-0.32 muM).
K252c (CAS 85753-43-1) References
- Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase. | Zimmermann, A., et al. 2000. Antiviral Res. 48: 49-60. PMID: 11080540
- Biological targets of antitumor indolocarbazoles bearing a sugar moiety. | Prudhomme, M. 2004. Curr Med Chem Anticancer Agents. 4: 509-21. PMID: 15579016
- Staurosporine and rebeccamycin aglycones are assembled by the oxidative action of StaP, StaC, and RebC on chromopyrrolic acid. | Howard-Jones, AR. and Walsh, CT. 2006. J Am Chem Soc. 128: 12289-98. PMID: 16967980
- Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a. | Hudkins, RL., et al. 2007. J Med Chem. 50: 433-41. PMID: 17266195
- Inhibition of ABCG2-mediated transport by protein kinase inhibitors with a bisindolylmaleimide or indolocarbazole structure. | Robey, RW., et al. 2007. Mol Cancer Ther. 6: 1877-85. PMID: 17575116
- Characterization and functional modification of StaC and RebC, which are involved in the pyrrole oxidation of indolocarbazole biosynthesis. | Asamizu, S., et al. 2011. Biosci Biotechnol Biochem. 75: 2184-93. PMID: 22056432
- Coupling of Ci-VSP modules requires a combination of structure and electrostatics within the linker. | Hobiger, K., et al. 2012. Biophys J. 102: 1313-22. PMID: 22455914
- Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. | Rüegg, UT. and Burgess, GM. 1989. Trends Pharmacol Sci. 10: 218-20. PMID: 2672462
- Induction of Gnrh mRNA expression by the ω-3 polyunsaturated fatty acid docosahexaenoic acid and the saturated fatty acid palmitate in a GnRH-synthesizing neuronal cell model, mHypoA-GnRH/GFP. | Tran, DQ., et al. 2016. Mol Cell Endocrinol. 426: 125-35. PMID: 26923440
- Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c. | Esvan, YJ., et al. 2016. Bioorg Med Chem. 24: 3116-24. PMID: 27255178
- Palmitate and Nitric Oxide Regulate the Expression of Spexin and Galanin Receptors 2 and 3 in Hypothalamic Neurons. | Tran, A., et al. 2020. Neuroscience. 447: 41-52. PMID: 31730796
- Antikinetoplastid Activity of Indolocarbazoles from Streptomyces sanyensis. | Cartuche, L., et al. 2020. Biomolecules. 10: PMID: 32344693
- K-252b, c and d, potent inhibitors of protein kinase C from microbial origin. | Nakanishi, S., et al. 1986. J Antibiot (Tokyo). 39: 1066-71. PMID: 3759658
- The structures of the novel protein kinase C inhibitors K-252a, b, c and d. | Yasuzawa, T., et al. 1986. J Antibiot (Tokyo). 39: 1072-8. PMID: 3759659
- Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. | Fabre, S., et al. 1993. Bioorg Med Chem. 1: 193-6. PMID: 8081852
Inhibitor of:
Chymotrypsin, LACTB, MDH1B, MDH2, MDHC, PKA, PKC, and Ser/Thr Protein Kinase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
K252c, 1 mg | sc-24011 | 1 mg | $87.00 | |||
K252c, 5 mg | sc-24011A | 5 mg | $374.00 |