GLPBio

Ryuvidine

Catalog No.: GC17150Purity:>95.00%Synonyms: Cdk4 Inhibitor III, Cyclic-dependent Kinase 4 Inhibitor III, SPS812
COASDSData Sheet
Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 value of 0.5µM.

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Ryuvidine
Cas No.: 265312-55-8
10mM (in 1mL DMSO)In Stock
$134.00
1
1mgIn Stock
$50.00
1
5mgIn Stock
$122.00
1
10mgIn Stock
$173.00
1
25mgIn Stock
$320.00
1
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Description

Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 value of 0.5µM [1]. Ryuvidine can strongly inhibit the activity of KDM5A (IC50=1.4μM) and block H3K4me3 demethylation [2]. Ryuvidine has been widely used to stabilize the Uhrf1 protein and to alleviate arthritis in mice [3].

In vitro, Ryuvidine treatment for 72 hours significantly inhibited the proliferation of HPV-negative Cal33 cells, and SCC15 cells, with IC50 values of 1.38μM and 1.17μM, respectively [4]. Treatment with 20μM Ryuvidine for 2 hours significantly induced phosphorylation of the CHK2 kinase at the threonine 68 site in HeLa cells, decreased the level of CDC7 and blocked DNA synthesis[5]. Treatment with 5μM Ryuvidine for 48 hours significantly inhibited apoptosis in human red blood cells after chloride ion removal, and reduced the exposure of phosphatidylserine (PS) on the cell membrane[6].

In vivo, Ryuvidine treatment via intraperitoneal injection at a dose of 0.8μg/g for 4 times within 5 days significantly alleviated the exacerbation of the arthritis phenotype in K/BxN serum transfer arthritis (STA) mice and reduced the serum Ccl20 level[7].

References:
[1] Blum G, Ibáñez G, Rao X, et al. Small-molecule inhibitors of SETD8 with cellular activity[J]. ACS chemical biology, 2014, 9(11): 2471-2478.
[2] Mitsui E, Yoshida S, Shinoda Y, et al. Identification of ryuvidine as a KDM5A inhibitor[J]. Scientific Reports, 2019, 9(1): 9952.
[3] Saeki N, Inoue K I, Ideta-Otsuka M I O, et al. Stabilization of UHRF1 in synovial fibroblasts is a novel therapeutic strategy for rheumatoid arthritis[J]. Bone Reports, 2022, 16: 101575.
[4] Ghasemi F, Black M, Sun R X, et al. High-throughput testing in head and neck squamous cell carcinoma identifies agents with preferential activity in human papillomavirus-positive or negative cell lines[J]. Oncotarget, 2018, 9(40): 26064.
[5] FitzGerald J, Murillo L S, O'Brien G, et al. A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response[J]. PLoS One, 2014, 9(6): e98891.
[6] Lang E, Zelenak C, Eberhard M, et al. Impact of cyclin-dependent kinase CDK4 inhibition on eryptosis[J]. Cellular physiology and biochemistry, 2015, 37(3): 1178-1186.
[7] Saeki N, Inoue K, Ideta-Otsuka M, et al. Epigenetic regulator UHRF1 orchestrates proinflammatory gene expression in rheumatoid arthritis in a suppressive manner[J]. The Journal of Clinical Investigation, 2022, 132(11).

Protocol

Cell experiment [1]:

Cell lines

SCC15 cells

Preparation Method

SCC15 cells were cultured in DMEM:Ham's F12 medium supplemented with 100μg/ml streptomycin, 100μg/ml penicillin and 10% fetal bovine serum at 37°C in an incubator with 5% CO2. Cells were seeded in 96-well plates at 3000 cells/well. After 24 hours, Ryuvidine was added at a concentration of 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30 and 100μM. Three technical replicates were carried out. Cells were incubated with the added Ryuvidine for 72 hours before assessing cell viability.

Reaction Conditions

0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30 and 100μM; 72h

Applications

Ryuvidine treatment inhibited cell viability of SCC15 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Female C57BL/6 mice

Preparation Method

Female C57BL/6 mice, aged 7 weeks with weights of 22-25g, were housed in cages and maintained in air-conditioned animal quarters with a 12h light-dark cycle and free access to autoclaved tap water and a standard chow diet. For STA induction, 50μl K/BxN serum was i.p. administered on days 0 and 3. A single 0.8μg/g dose of Ryuvidine in DMSO and corn oil (16μl/g) was i.p. administered on days 1, 2, 4, and 5 for STA mice. The phenotypic characteristics of arthritis and the histopathological features of the synovium in mice were analyzed within 10 days.

Dosage form

0.8μg/g; 4 times within 5 days; i.p.

Applications

Ryuvidine treatment delayed exacerbation of arthritis phenotypes and inhibited synovial hyperplasia in STA mice.

References:
[1] Ghasemi F, Black M, Sun R X, et al. High-throughput testing in head and neck squamous cell carcinoma identifies agents with preferential activity in human papillomavirus-positive or negative cell lines[J]. Oncotarget, 2018, 9(40): 26064.
[2] Saeki N, Inoue K, Ideta-Otsuka M, et al. Epigenetic regulator UHRF1 orchestrates proinflammatory gene expression in rheumatoid arthritis in a suppressive manner[J]. The Journal of Clinical Investigation, 2022, 132(11).

Product Documents

Purity:>95.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
265312-55-8
Synonyms
Cdk4 Inhibitor III, Cyclic-dependent Kinase 4 Inhibitor III, SPS812
Chemical Name
2-methyl-5-(p-tolylamino)benzo[d]thiazole-4,7-dione
SMILES
O=C(C1=C2SC(C)=N1)C(NC3=CC=C(C)C=C3)=CC2=O
Molecular Formula
C15H12N2O2S
Molecular Weight
284.33
Solubility
DMF: 5 mg/ml,DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml,DMSO: 2 mg/ml,Ethanol: 0.5 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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