Ryuvidine
Based on 1 Customer Validation
Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.23%
- CAS 番号: 265312-55-8
- 分子式: C15H12N2O2S
- 分子量:284.33
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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CDK4 6.0 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.61 mg/mL
Compound: K00601a, Benzothiazole1
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Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
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[PMID: 18077363] |
| A549 | IC50 |
0.61 μg/mL
Compound: 5g
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Inhibition of A549 cancer cell proliferation
Inhibition of A549 cancer cell proliferation
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[PMID: 10743948] |
| COLO1 | IC50 |
1.08 μg/mL
Compound: 5g
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Inhibition of Col1 cancer cell proliferation
Inhibition of Col1 cancer cell proliferation
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[PMID: 10743948] |
| HeLa | IC50 |
0.37 μM
Compound: Ryuvidine
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Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr
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[PMID: 35525212] |
| HepG2 | IC50 |
1.2 μg/mL
Compound: 4d
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In vitro cytotoxicity against HepG2 cells (Hepatocarcinoma from ATCC) by MTT assay
In vitro cytotoxicity against HepG2 cells (Hepatocarcinoma from ATCC) by MTT assay
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[PMID: 10915058] |
| HepG2 | IC50 |
1.21 mg/mL
Compound: K00601a, Benzothiazole1
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Antitumor activity against human HepG2 cells
Antitumor activity against human HepG2 cells
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[PMID: 18077363] |
| HepG2 | IC50 |
1.21 μg/mL
Compound: 5g
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Inhibition of HepG2 cancer cell proliferation
Inhibition of HepG2 cancer cell proliferation
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[PMID: 10743948] |
| HL-60 | IC50 |
0.3 mg/mL
Compound: K00601a, Benzothiazole1
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Antitumor activity in human HL60 cells
Antitumor activity in human HL60 cells
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[PMID: 18077363] |
| HL-60 | IC50 |
0.3 μg/mL
Compound: 5g
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Inhibition of HL60 cancer cell proliferation
Inhibition of HL60 cancer cell proliferation
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[PMID: 10743948] |
| Sf9 | IC50 |
>20 μM
Compound: Ryuvidine
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Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
>20 μM
Compound: Ryuvidine
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Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
>20 μM
Compound: Ryuvidine
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Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
>20 μM
Compound: Ryuvidine
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Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
>20 μM
Compound: Ryuvidine
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Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
9.5 μM
Compound: Ryuvidine
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Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
体外実験
Ryuvidine (1-20 µM, 1-9 h) reduces CDC7 levels and blocks DNA synthesis in HeLa cells[3].
Ryuvidine (48 h) strongly inhibits KAIMRC2 (a breast cancer cell line) cell growth at an IC50 value of 0.8 µM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:1, 5, 10, 20 µM
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Incubation Time:1, 3, 6, 9
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Result:Decreased pSer40/41 MCM2 and CDC7 protein levels.
Did not obviously affect the adjacent CDC7-independent phosphorylation of Ser41.
Completely dephosphorylated MCM2 at 20 µM.
体内実験
化学情報
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CAS 番号 265312-55-8
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性状 Solid
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分子量 284.33
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分子式 C15H12N2O2S
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Color Brown to black
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SMILES
O=C1C=C(C(C2=C1SC(C)=N2)=O)NC3=CC=C(C)C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (43.96 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ryu CK, et al. 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg Med Chem Lett. 2000 Mar 6;10(5):461-4. [Content Brief]
[2]. Blum G, et al. Small-molecule inhibitors of SETD8 with cellular activity. ACS Chem Biol. 2014 Nov 21;9(11):2471-8. [Content Brief]
[3]. FitzGerald J, et al. 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. [Content Brief]
[4]. Ali R, et al. Isolation and Establishment of a Highly Proliferative, Cancer Stem Cell-Like, and Naturally Immortalized Triple-Negative Breast Cancer Cell Line, KAIMRC2. Cells. 2021 May 24;10(6):1303. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5170 mL | 17.5852 mL | 35.1704 mL | 87.9260 mL |
| 5 mM | 0.7034 mL | 3.5170 mL | 7.0341 mL | 17.5852 mL | |
| 10 mM | 0.3517 mL | 1.7585 mL | 3.5170 mL | 8.7926 mL | |
| 15 mM | 0.2345 mL | 1.1723 mL | 2.3447 mL | 5.8617 mL | |
| 20 mM | 0.1759 mL | 0.8793 mL | 1.7585 mL | 4.3963 mL | |
| 25 mM | 0.1407 mL | 0.7034 mL | 1.4068 mL | 3.5170 mL | |
| 30 mM | 0.1172 mL | 0.5862 mL | 1.1723 mL | 2.9309 mL | |
| 40 mM | 0.0879 mL | 0.4396 mL | 0.8793 mL | 2.1982 mL |
Ryuvidine 関連分類
HY-100624 関連分類
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