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Submit ReviewPotent cyclin-dependent kinase 4 (cdk4) inhibitor (IC50 value reported between 60 and 190 nM). Displays activity at other cdks in the sub-micromolar range. Also potently inhibits CaM kinase II (IC50 = 25 nM). Inhibits human cytomegalovirus (HCMV) replication in vitro.
Arcyriaflavin A is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 325.32 |
Formula | C20H11N3O2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 118458-54-1 |
PubChem ID | 5327723 |
InChI Key | KAJXOWFGKYKMMZ-UHFFFAOYSA-N |
Smiles | O=C1NC(=O)C2=C1C1=C(NC3=CC=CC=C13)C1=C2C2=C(N1)C=CC=C2 |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 32.53 | 100 |
The following data is based on the product molecular weight 325.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.07 mL | 15.37 mL | 30.74 mL |
5 mM | 0.61 mL | 3.07 mL | 6.15 mL |
10 mM | 0.31 mL | 1.54 mL | 3.07 mL |
50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
References are publications that support the biological activity of the product.
Slater et al (1999) Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication. Bioorg.Med.Chem. 7 1067 PMID: 10428375
Zhu et al (2003) Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. Bioorg.Med.Chem.Lett. 13 1231 PMID: 12657252
Sanchez-Martinez et al (2003) Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. Bioorg.Med.Chem.Lett. 13 3835 PMID: 14552791
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
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Keywords: Arcyriaflavin A, Arcyriaflavin A supplier, Potent, CaM, Kinase, II, cdk4, cyclin, D1, inhibitors, inhibits, Antiviral, agent, anti-HCMV, Calmodulin-Activated, calmodulin-dependent, Protein, Kinases, Cdk, Cyclin-Dependent, Ca2+, Binding, modulators, Calmodulin, Calcium, Signaling, Signalling, ArcyriaflavinA, Cyclin-dependent, Cytomegalovirus, 2457, Tocris Bioscience
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Arcyriaflavin A was observed for its activity on cell viability, proliferation, and angiogenesis of ECSCs as assessed using the 5-bromo-2-deoxyuridine (BrdU) and methylthiazoletetrazolium bromide (MTT) assays, and vascular endothelial growth factor (VEGF) ELISA.
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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.