Ryuvidine

Ryuvidine is a potent inhibitor of SET domain-containing protein 8 (SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis[1][2][3][4][5].

Product Specifications

CAS Number

[265312-55-8]

UNSPSC

12352005

Target

CDK; DNA/RNA Synthesis; Histone Demethylase; Histone Methyltransferase

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ryuvidine.html

Purity

99.40

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C=C(C(C2=C1SC(C)=N2)=O)NC3=CC=C(C)C=C3

Molecular Formula

C15H12N2O2S

Molecular Weight

284.33

References & Citations

[1]Ryu CK, et al. 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg Med Chem Lett. 2000 Mar 6;10 (5) :461-4. |[2]Blum G, et al. Small-molecule inhibitors of SETD8 with cellular activity. ACS Chem Biol. 2014 Nov 21;9 (11) :2471-8. |[3]FitzGerald J, et al. A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response. PLoS One. 2014 Jun 5;9 (6) :e98891.|[4]Ali R, et al. Isolation and Establishment of a Highly Proliferative, Cancer Stem Cell-Like, and Naturally Immortalized Triple-Negative Breast Cancer Cell Line, KAIMRC2. Cells. 2021 May 24;10 (6) :1303.|[5]Cotti S, et al. More bone with less minerals: the effects of dietary phosphorus on the zebrafish skeleton[C]//49th European Calcified Tissue Society Congress (ECTS 2022) . 2022, 16: 59-60.