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Submit ReviewRyuvidine
Description: SETD8 inhibitor; also CDK4 inhibitor
Chemical Name: 2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione
Purity: ≥98% (HPLC)
Biological Activity for Ryuvidine
Ryuvidine is an 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 for Ryuvidine
Ryuvidine is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Ryuvidine
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ryuvidine
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.69 | 20 | |
| ethanol | 1.42 | 5 |
Preparing Stock Solutions for Ryuvidine
The following data is based on the product molecular weight 284.33. 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 |
|---|---|---|---|
| 0.2 mM | 17.59 mL | 87.93 mL | 175.85 mL |
| 1 mM | 3.52 mL | 17.59 mL | 35.17 mL |
| 2 mM | 1.76 mL | 8.79 mL | 17.59 mL |
| 10 mM | 0.35 mL | 1.76 mL | 3.52 mL |
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Product Datasheets for Ryuvidine
References for Ryuvidine
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Ryuvidine, please let us know.
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Keywords: Ryuvidine, Ryuvidine supplier, Cyclin-dependent, protein, kinase, 4, cdk4, inhibitors, SETD8, lysine, methyltransferases, inhibits, SPS8I2, Kinase, Lysine, Methyltransferases, Other, CDK4, Subfamily, 2609, Tocris Bioscience
1 Citation for Ryuvidine
Citations are publications that use Tocris products. Selected citations for Ryuvidine include:
FitzGerald et al (2014) A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response. PLoS One 9 e98891 PMID: 24902048
Do you know of a great paper that uses Ryuvidine from Tocris? Please let us know.
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