Ryuvidine - CAS 265312-55-8
Category: Inhibitor
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Ryuvidine, a cell-permeable dioxobenzothiazole compound, is an inhibitor of SETD8 (IC50 = 0.5 µM) that suppresses monomethylation of H4K20 in vitro.1 It less potently inhibits cyclin-dependent kinase 4 (Cdk4; IC50 = 6 µM for Cdk4/cyclin D1).
≥98% by HPLC
2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione; Cdk4 Inhibitor III; Cyclic-dependent Kinase 4 Inhibitor III; Ryuvidine; SPS8I2; SPS-8I2; SPS 8I2;
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.High-throughput testing in head and neck squamous cell carcinoma identifies agents with preferential activity in human papillomavirus-positive or negative cell lines.
Ghasemi F;Black M;Sun RX;Vizeacoumar F;Pinto N;Ruicci KM;Yoo J;Fung K;MacNeil D;Palma DA;Winquist E;Mymryk JS;Ailles LA;Datti A;Barrett JW;Boutros PC;Nichols AC Oncotarget. 2018 May 25;9(40):26064-26071. doi: 10.18632/oncotarget.25436. eCollection 2018 May 25.
Head and neck squamous cell carcinoma (HNSCC) is a common cancer diagnosis worldwide. Despite advances in treatment, HNSCC has very poor survival outcomes, emphasizing an ongoing need for development of improved therapeutic options. The distinct tumor characteristics of human papillomavirus (HPV)-positive ;vs;. HPV-negative disease necessitate development of treatment strategies tailored to tumor HPV-status. High-throughput robotic screening of 1,433 biologically and pharmacologically relevant compounds at a single dose (4 μM) was carried out against 6 HPV-positive and 20 HPV-negative HNSCC cell lines for preliminary identification of therapeutically relevant compounds. Statistical analysis was further carried out to differentiate compounds with preferential activity against cell lines stratified by the HPV-status. These analyses yielded 57 compounds with higher activity in HPV-negative cell lines, and 34 with higher-activity in HPV-positive ones. Multi-point dose-response curves were generated for six of these compounds (Ryuvidine, MK-1775, SNS-032, Flavopiridol, AZD-7762 and ARP-101), confirming Ryuvidine to have preferential potency against HPV-negative cell lines, and MK-1775 to have preferential potency against HPV-positive cell lines.
2.Sensitivity Profiles of Human Prostate Cancer Cell Lines to an 80 Kinase Inhibitor Panel.
Burke AJ;Ali H;O'Connell E;Sullivan FJ;Glynn SA Anticancer Res. 2016 Feb;36(2):633-41.
BACKGROUND: ;Taxanes and anti-androgen therapies are routinely used for the treatment of metastatic prostate cancer, however the majority of patients eventually develop resistance.;MATERIALS AND METHODS: ;Eighty kinase inhibitors were screened regarding their ability to inhibit cell viability in CWR22, 22Rv1, PC-3 and DU145 prostate cancer cells using automated toxicity assays. Four kinase inhibitors were selected for further investigation.;RESULTS: ;No significant difference in sensitivity patterns was found between the androgen receptor wild-type CWR22 and its androgen receptor mutant variant 22Rv1, indicating that androgen receptor mutation did not impact on kinase inhibitor sensitivity in this model. Metastatic PC-3 and DU145 prostate cancer cell lines were less sensitive to kinase inhibitors than the non-metastatic CWR22 and 22Rv1. All four cell lines responded to GSK-3 inhibitor BIO, and MEK inhibitor PD198306. DU145 cells were resistant to p75NTR/TrkA and CHK4 inhibitors, RO-082750 and Ryuvidine.;CONCLUSION: ;Kinase inhibition may be an appropriate strategy for the treatment of prostate cancer.;Copyright© 2016 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.
3.Small-molecule inhibitors of SETD8 with cellular activity.
Blum G;Ibáñez G;Rao X;Shum D;Radu C;Djaballah H;Rice JC;Luo M ACS Chem Biol. 2014 Nov 21;9(11):2471-8. doi: 10.1021/cb500515r. Epub 2014 Sep 3.
SETD8/SET8/Pr-SET7/KMT5A is the sole protein lysine methyltransferase (PKMT) known to monomethylate lysine 20 of histone H4 in vivo. SETD8's methyltransferase activity has been implicated in many essential cellular processes including DNA replication, DNA damage response, transcription modulation, and cell cycle regulation. Developing SETD8 inhibitors with cellular activity is a key step toward elucidating the diverse roles of SETD8 via convenient pharmacological perturbation. From the hits of a prior high throughput screen (HTS), SPS8I1-3 (NSC663284, BVT948, and ryuvidine) were validated as potent SETD8 inhibitors. These compounds contain different structural motifs and inhibit SETD8 via distinct modes. More importantly, these compounds show cellular activity by suppressing the H4K20me1 mark of SETD8 and recapitulate characteristic S/G2/M-phase cell cycle defects as observed for RNAi-mediated SETD8 knockdown. The commonality of SPS8I1-3 against SETD8, together with their distinct structures and mechanisms for SETD8 inhibition, argues for the collective application of these compounds as SETD8 inhibitors.
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CAS 265312-55-8 Ryuvidine

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