Ryuvidine (Synonyms: Cdk4 Inhibitor III, Cyclic-dependent Kinase 4 Inhibitor III, SPS812) |
カタログ番号GC17150
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リュビジンは、IC50 が 0.5 μM の SET ドメイン含有タンパク質 8(SETD8) の強力な阻害剤であり、in vitro で H4K20 のモノメチル化を抑制します。リュビジンはまた、6.0 μM の IC50 で CDK4 を阻害し、さまざまなヒト癌細胞に対して細胞毒性を示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 265312-55-8
Sample solution is provided at 25 µL, 10mM.
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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).
| 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: | |
| Cas No. | 265312-55-8 | SDF | |
| 同義語 | Cdk4 Inhibitor III, Cyclic-dependent Kinase 4 Inhibitor III, SPS812 | ||
| Chemical Name | 2-methyl-5-(p-tolylamino)benzo[d]thiazole-4,7-dione | ||
| Canonical SMILES | O=C(C1=C2SC(C)=N1)C(NC3=CC=C(C)C=C3)=CC2=O | ||
| Formula | C15H12N2O2S | M.Wt | 284.33 |
| 溶解度 | 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 | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.517 mL | 17.5852 mL | 35.1704 mL |
| 5 mM | 703.4 μL | 3.517 mL | 7.0341 mL |
| 10 mM | 351.7 μL | 1.7585 mL | 3.517 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00% Appearance: A solid
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- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)