Ryuvidine | CAS#265312-55-8 | SETD8 inhibitor

MedKoo Cat#: 562812 | Name: Ryuvidine

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ryuvidine is an inhibitor of SETD8 with cellular activity. It also acts as a CDK4 inhibitor and inducer of the DNA damage response.

Chemical Structure

Ryuvidine

CAS#265312-55-8

Theoretical Analysis

MedKoo Cat#: 562812

Name: Ryuvidine

CAS#: 265312-55-8

Chemical Formula: C15H12N2O2S

Exact Mass: 284.0619

Molecular Weight: 284.33

Elemental Analysis: C, 63.36; H, 4.25; N, 9.85; O, 11.25; S, 11.28

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 400.00
10mg	USD 650.00

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Synonym

Ryuvidine; SPS8I2; SPS-8I2; SPS 8I2;

IUPAC/Chemical Name

2-methyl-5-(p-tolylamino)benzo[d]thiazole-4,7-dione

InChi Key

HFPLHASLIOXVGS-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H12N2O2S/c1-8-3-5-10(6-4-8)17-11-7-12(18)15-13(14(11)19)16-9(2)20-15/h3-7,17H,1-2H3

SMILES Code

CC1=NC2=C(C(C=C(NC3=CC=C(C)C=C3)C2=O)=O)S1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Ryuvidine is an inhibitor of SETD8 PKMT (IC50 = 0.5 μM) and suppresses H4K20 monomethylation in vitro. Ryuvidine inhibits CDK4 (IC50 = 6.0 μM at CDK4/cyclin D1). Ryuvidine induces S phase accumulation in HEK293T cells.

In vitro activity:

Through high-throughput robotic screening against HPV-positive and HPV-negative HNSCC cell lines, Ryuvidine emerged as a compound with preferential potency against HPV-negative cell lines. Ryuvidine may hold promise as a potential therapeutic agent tailored to the specific tumor characteristics of HPV-negative HNSCC. Reference: Oncotarget. 2018 May 25;9(40):26064-26071. https://pubmed.ncbi.nlm.nih.gov/29899842/

In vivo activity:

Ryuvidine administration led to the stabilization of UHRF1 and ameliorated arthritis pathogeneses in a mouse model of rheumatoid arthritis. These findings suggest that targeting UHRF1 could be a promising therapeutic strategy for Rheumatoid arthritis, meaning Ryuvidine could be a potential candidate for Rheumatoid arthritis treatment. Reference: J Clin Invest. 2022 Jun 1;132(11):e150533. https://pubmed.ncbi.nlm.nih.gov/35472067/

	Solvent	mg/mL	mM
Solubility
	DMSO	5.7	20.00
	Ethanol	1.4	5.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 284.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. 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. High-throughput testing in head and neck squamous cell carcinoma identifies agents with preferential activity in human papillomavirus-positive or negative cell lines. Oncotarget. 2018 May 25;9(40):26064-26071. doi: 10.18632/oncotarget.25436. PMID: 29899842; PMCID: PMC5995257. 2. FitzGerald J, Murillo LS, O'Brien G, O'Connell E, O'Connor A, Wu K, Wang GN, Rainey MD, Natoni A, Healy S, O'Dwyer M, Santocanale C. 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. doi: 10.1371/journal.pone.0098891. PMID: 24902048; PMCID: PMC4047068. 3. Saeki N, Inoue K, Ideta-Otsuka M, Watamori K, Mizuki S, Takenaka K, Igarashi K, Miura H, Takeda S, Imai Y. Epigenetic regulator UHRF1 orchestrates proinflammatory gene expression in rheumatoid arthritis in a suppressive manner. J Clin Invest. 2022 Jun 1;132(11):e150533. doi: 10.1172/JCI150533. PMID: 35472067; PMCID: PMC9151705.

In vitro protocol:

In vivo protocol:

1. Saeki N, Inoue K, Ideta-Otsuka M, Watamori K, Mizuki S, Takenaka K, Igarashi K, Miura H, Takeda S, Imai Y. Epigenetic regulator UHRF1 orchestrates proinflammatory gene expression in rheumatoid arthritis in a suppressive manner. J Clin Invest. 2022 Jun 1;132(11):e150533. doi: 10.1172/JCI150533. PMID: 35472067; PMCID: PMC9151705.

1: Lewandrowski KU, Sharafshah A, Elfar J, Schmidt SL, Blum K, Wetzel FT. A Pharmacogenomics-Based In Silico Investigation of Opioid Prescribing in Post- operative Spine Pain Management and Personalized Therapy. Cell Mol Neurobiol. 2024 May 27;44(1):47. doi: 10.1007/s10571-024-01466-5. PMID: 38801645; PMCID: PMC11129978. 2: Liu X, Shen X, Wang H, Wang J, Ren Y, Zhang M, Li S, Guo L, Li J, Wang Y. Mollugin prevents CLP-induced sepsis in mice by inhibiting TAK1-NF-κB/MAPKs pathways and activating Keap1-Nrf2 pathway in macrophages. Int Immunopharmacol. 2023 Dec;125(Pt A):111079. doi: 10.1016/j.intimp.2023.111079. Epub 2023 Oct 27. PMID: 38149576. 3: Wang W, Zhou L, Zhang X, Li Z. Mollugin suppresses proliferation and drives ferroptosis of colorectal cancer cells through inhibition of insulin-like growth factor 2 mRNA binding protein 3/glutathione peroxidase 4 axis. Biomed Pharmacother. 2023 Oct;166:115427. doi: 10.1016/j.biopha.2023.115427. Epub 2023 Sep 5. PMID: 37677963. 4: Wang Z, Cui X, Yan W, Liu N, Shang J, Yi X, Guo T, Wei X, Sun Y, Hu H, Ma W, Cui W, Chen L. Mollugin activates GLP-1R to improve cognitive dysfunction in type 2 diabetic mice. Life Sci. 2023 Oct 15;331:122026. doi: 10.1016/j.lfs.2023.122026. Epub 2023 Aug 21. PMID: 37607641. 5: Li X, Hou R, Ding H, Gao X, Wei Z, Qi T, Fang L. Mollugin ameliorates murine allergic airway inflammation by inhibiting Th2 response and M2 macrophage activation. Eur J Pharmacol. 2023 May 5;946:175630. doi: 10.1016/j.ejphar.2023.175630. Epub 2023 Mar 4. PMID: 36871665. 6: Zhang LH, Li MY, Wang DY, Jin XJ, Chen FE, Piao HR. Synthesis and Evaluation of NF-κB Inhibitory Activity of Mollugin Derivatives. Molecules. 2022 Nov 16;27(22):7925. doi: 10.3390/molecules27227925. PMID: 36432026; PMCID: PMC9695821. 7: Ke XG, Xiong YY, Yu B, Yuan C, Chen PY, Yang YF, Wu HZ. Mollugin induced oxidative DNA damage via up-regulating ROS that caused cell cycle arrest in hepatoma cells. Chem Biol Interact. 2022 Feb 1;353:109805. doi: 10.1016/j.cbi.2022.109805. Epub 2022 Jan 8. PMID: 35007525. 8: Luo H, Lv YF, Zhang H, Hu JM, Li HM, Liu SJ. Synthesis and Antitumor Activity of 1-Substituted 1,2,3-Triazole-Mollugin Derivatives. Molecules. 2021 May 28;26(11):3249. doi: 10.3390/molecules26113249. PMID: 34071319; PMCID: PMC8198100. 9: Zeng L, Xu T, Meng J, Wu D, Wu S. H2O-Induced Hydrophobic Interactions in MS-Guided Counter-Current Chromatography Separation of Anti- Cancer Mollugin from Rubia cordifolia. Molecules. 2021 Feb 2;26(3):751. doi: 10.3390/molecules26030751. PMID: 33540504; PMCID: PMC7867130. 10: Li J, Zhang JL, Gong XP, Xiao M, Song YY, Pi HF, Du G. Anti-inflammatory Activity of Mollugin on DSS-induced Colitis in Mice. Curr Med Sci. 2020 Oct;40(5):910-916. doi: 10.1007/s11596-020-2262-5. Epub 2020 Oct 29. PMID: 33123905. 11: Yan W, Jiang Z, Fan F. Analgesic action of Rubimaillin in vitro and in vivo. Cell Mol Biol (Noisy-le-grand). 2020 Jun 5;66(3):171-175. PMID: 32538766. 12: Cai F, Guo S, Huang S, Li J, Liu W. Rubimaillin suppresses proliferation, migration and invasion of prostate cancer cells via the Notch-1/MMP signaling pathway. Cell Mol Biol (Noisy-le-grand). 2020 May 15;66(2):130-134. PMID: 32415939. 13: Siwei Z, Zhen W, Zhi Z, Xuguang H, Yousheng L. Rubimaillin decreases the viability of human ovarian cancer cells via mitochondria-dependent apoptosis. Cell Mol Biol (Noisy-le-grand). 2019 Sep 30;65(7):72-76. PMID: 31880521. 14: Zhang Y, Zhou S, Zhou J, Wang D, Zhou T. Regulation of NF-κB/MAPK signaling pathway attenuates the acute lung inflammation in Klebsiella pneumonia rats by mollugin treatment. Microb Pathog. 2019 Jul;132:369-373. doi: 10.1016/j.micpath.2019.05.007. Epub 2019 May 8. PMID: 31075430. 15: Hong KB, Kim D, Kim BK, Woo SY, Lee JH, Han SH, Bae GU, Kang S. CF₃- Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti- inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability. Molecules. 2018 Aug 14;23(8):2030. doi: 10.3390/molecules23082030. PMID: 30110934; PMCID: PMC6222789. 16: Moon SH, Kim I, Kim SH. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway. Arch Pharm Res. 2017 Nov;40(11):1328-1335. doi: 10.1007/s12272-017-0964-4. Epub 2017 Oct 12. PMID: 29027119. 17: Xu L, Cao GS, Wang X, Li WM, Shi W, Li PP, Zhang F, Li YN. [Preparation and in vitro release evaluation of slow releasing intrauterine silicone rubber bar made of Panax notoginseng and Rubia cordifolia]. Zhongguo Zhong Yao Za Zhi. 2017 Jan;42(1):113-118. Chinese. doi: 10.19540/j.cnki.cjcmm.20161222.036. PMID: 28945034. 18: Wang Z, Li MY, Mi C, Wang KS, Ma J, Jin X. Mollugin Has an Anti-Cancer Therapeutic Effect by Inhibiting TNF-α-Induced NF-κB Activation. Int J Mol Sci. 2017 Jul 26;18(8):1619. doi: 10.3390/ijms18081619. PMID: 28933726; PMCID: PMC5578011. 19: Gao M, Yang J, Wang Z, Yang B, Kuang H, Liu L, Wang L, Yang C. Simultaneous Determination of Purpurin, Munjistin and Mollugin in Rat Plasma by Ultra High Performance Liquid Chromatography-Tandem Mass Spectrometry: Application to a Pharmacokinetic Study after Oral Administration of Rubia cordifolia L. Extract. Molecules. 2016 Jun 1;21(6):717. doi: 10.3390/molecules21060717. PMID: 27258244; PMCID: PMC6273328. 20: Yang HS, Wang J, Guo C, Liu W, Chen YY, Wei JF, Kang WY. Simultaneous determination of alizarin and rubimaillin in Rubia cordifolia by ultrasound- assisted ionic liquid-reversed phase liquid chromatography. Zhongguo Zhong Yao Za Zhi. 2015 Jul;40(13):2617-23. PMID: 26697688.