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Submit ReviewK-252c is an inhibitor of protein kinase C (IC50 = 2.45 μM) that displays ~ 10-fold selectivity over protein kinase A (IC50 = 25.7 μM). Also inhibits β-lactamase, malate dehydrogenase and chymotrypsin (IC50 values are 8, 8 and 10 μM respectively). Exhibits antiviral activity against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) (IC50 values range from 0.13 - 0.32 μM). Shows no activity against herpes simplex virus (HSV).
M. Wt | 311.34 |
Formula | C20H13N3O |
Storage | Store at -20°C |
Purity | ≥99% (HPLC) |
CAS Number | 85753-43-1 |
PubChem ID | 3815 |
InChI Key | MEXUTNIFSHFQRG-UHFFFAOYSA-N |
Smiles | O=C(NC3)C1=C3C(C4=CC=CC=C4N5)=C5C2=C1C6=C(C=CC=C6)N2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Fabre et al (1993) Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg.Med.Chem. 1 193 PMID: 8081852
Zimmermann et al (2000) Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase. Antiviral Res. 48 49 PMID: 11080540
McGovern and Shoichet (2003) Kinase inhibitors: not just for kinases anymore. J.Med.Chem. 46 1478 PMID: 12672248
Keywords: K-252c, K-252c supplier, Protein, kinases, C, inhibitors, inhibits, PKC, Staurosporinone, Kinase, Cytomegalovirus, 2287, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for K-252c include:
Goldman et al (2012) An unusual role for a mobile flavin in StaC-like indolocarbazole biosynthetic enzymes. Chem Biol 19 855 PMID: 22840773
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