Biological Activity
Inhibitor of SETD8 protein lysine methyltransferase (PKMT) (IC50 = 0.5 μM); suppresses H4K20 monomethylation in vitro. Also inhibits cyclin-dependent kinase (CDK) 4 (IC50 = 6.0 μM at CDK4/cyclin D1). Induces S phase accumulation in HEK293T cells. Cytotoxic against a range of human cancer cells.
Compound Libraries
Ryuvidine is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 284.33 |
| Formula | C15H12N2O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 265312-55-8 |
| PubChem ID | 481747 |
| InChI Key | HFPLHASLIOXVGS-UHFFFAOYSA-N |
| Smiles | CC1=NC2=C(S1)C(=O)C=C(NC1=CC=C(C)C=C1)C2=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.69 | 20 | |
| ethanol | 1.42 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 284.33. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 3.52 mL | 17.59 mL | 35.17 mL |
| 5 mM | 0.7 mL | 3.52 mL | 7.03 mL |
| 10 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ryu et al (2000) 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg.Med.Chem.Lett. 10 461 PMID: 10743948
Blum et al (2014) Small-molecule inhibitors of SETD8 with cellular activity. ASC.Chem.Biol. [Epub ahead of print] 9 2471 PMID: 25137013
Keywords: Ryuvidine, supplier, Cyclin-dependent, protein, kinase, 4, cdk4, inhibitors, SETD8, protein, lysine, methyltransferases, inhibits, SPS8I2, Cyclin-dependent, Kinase, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
