RyuvidineSETD8 inhibitor; also CDK4 inhibitor CAS# 265312-55-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 265312-55-8 | SDF | Download SDF |
| PubChem ID | 481747 | Appearance | Powder |
| Formula | C15H12N2O2S | M.Wt | 284.33 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 20 mM in DMSO and to 5 mM in ethanol | ||
| Chemical Name | 2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione | ||
| SMILES | CC1=CC=C(C=C1)NC2=CC(=O)C3=C(C2=O)N=C(S3)C | ||
| Standard InChIKey | HFPLHASLIOXVGS-UHFFFAOYSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Inhibitor of SETD8 protein lysine methyltransferase (PKMT) (IC50 = 0.5 μM); suppresses H4K20 monomethylation in vitro. Also inhibits cyclin-dependent kinase (CDK) 4 (IC50 = 6.0 μM at CDK4/cyclin D1). Induces S phase accumulation in HEK293T cells. Cytotoxic against a range of human cancer cells. |
Ryuvidine Dilution Calculator
Ryuvidine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.517 mL | 17.5852 mL | 35.1704 mL | 70.3408 mL | 87.926 mL |
| 5 mM | 0.7034 mL | 3.517 mL | 7.0341 mL | 14.0682 mL | 17.5852 mL |
| 10 mM | 0.3517 mL | 1.7585 mL | 3.517 mL | 7.0341 mL | 8.7926 mL |
| 50 mM | 0.0703 mL | 0.3517 mL | 0.7034 mL | 1.4068 mL | 1.7585 mL |
| 100 mM | 0.0352 mL | 0.1759 mL | 0.3517 mL | 0.7034 mL | 0.8793 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response.[Pubmed:24902048]
PLoS One. 2014 Jun 5;9(6):e98891.
DNA replication is an essential process for cell division and as such it is a process that is directly targeted by several anticancer drugs. CDC7 plays an essential role in the activation of replication origins and has recently been proposed as a novel target for drug discovery. The MCM DNA helicase complex (MCM2-7) is a key target of the CDC7 kinase, and MCM phosphorylation status at specific sites is a reliable biomarker of CDC7 cellular activity. In this work we describe a cell-based assay that utilizes the "In Cell Western Technique" (ICW) to identify compounds that affect cellular CDC7 activity. By screening a library of approved drugs and kinase inhibitors we found several compounds that can affect CDC7-dependent phosphorylation of MCM2 in HeLa cells. Among these, Mitoxantrone, a topoisomerase inhibitor, and Ryuvidine, previously described as a CDK4 inhibitor, cause a reduction in phosphorylated MCM2 levels and a sudden blockade of DNA synthesis that is accompanied by an ATM-dependent checkpoint response. This study sheds light on the previously observed cytotoxity of Ryuvidine, strongly suggesting that it is related to its effect of causing DNA damage.
Small-molecule inhibitors of SETD8 with cellular activity.[Pubmed:25137013]
ACS Chem Biol. 2014 Nov 21;9(11):2471-8.
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.
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.[Pubmed:10743948]
Bioorg Med Chem Lett. 2000 Mar 6;10(5):461-4.
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles were synthesized as inhibitors of cyclin-dependent kinase 4 (CDK4) and cytotoxic agents. Most of the 4,7-dioxobenzothiazoles exhibited selective inhibitory activities for the CDK4 and cytotoxic potential against human cancer cell lines.
