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Ryuvidine

Catalog #: 2609
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Ryuvidine | CAS No. 265312-55-8 | Lysine Methyltransferase Inhibitors
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Description: SETD8 inhibitor; also CDK4 inhibitor

Chemical Name: 2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione

Purity: ≥98%

Product Details
Citations (1)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
284.33
Formula:
C15H12N2O2S
Solubility:
Soluble to 20 mM in DMSO and to 5 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
265312-55-8

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.

Background References

  1. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2
    NP Coussens, SC Kales, MJ Henderson, OW Lee, KY Horiuchi, Y Wang, Q Chen, E Kuznetsova, J Wu, S Chakka, DM Cheff, K Chih-Chien, P Shinn, KR Brimacombe, M Shen, A Simeonov, M Lal-Nag, H Ma, A Jadhav, MD Hall
    J. Biol. Chem., 2018;0(0):.
  2. Small-molecule inhibitors of SETD8 with cellular activity.
    Blum et al.
    ASC.Chem.Biol. [Epub ahead of print], 2014;9:2471
  3. 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.
    Ryu et al.
    Bioorg.Med.Chem.Lett., 2000;10:461

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Citation for Ryuvidine

The citations listed below are publications that use Tocris products. Selected citations for Ryuvidine include:

1 Citation: Showing 1 - 1

  1. A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response.
    Authors: FitzGerald Et al.
    PLoS One  2014;9:e98891

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