YM281
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma.
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- CAS No.: 2230914-84-6
- Formule: C56H71N7O9S
- Masse moléculaire:1018.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
5.4 μM
Compound: YM281
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Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
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[PMID: 38295690] |
| MV4-11 | IC50 |
>10 μM
Compound: YM281
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Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
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[PMID: 38295690] |
| RS4-11 | IC50 |
4.07 μM
Compound: YM281
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Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay
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[PMID: 38295690] |
YM281 (compound V2) (0-6 µM; 0-48 h) decreases the EZH2 protein level and the PRC2 (polycomb repressive complex 2) complex through the VHL (vonHippel−Lindau)-dependent ubiquitin-proteasome system[1].
YM281 (0-10 µM; 24 h) shows anticancer effects in lymphoma cells[1].
YM281 (0-5 µM) induces cell apoptosis and cell cycle arrest at the G0/G1 phase[1].
YM281 (0-5 µM; 24 h) increases the activity of caspase-3 and -7 and meanwhile reduces the cell viability in primary lymphoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DHL-2, 22Rv1 cells
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Concentration:0-6 µM
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Incubation Time:0-48 h
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Result:Abrogated both the EZH2 protein level and the H3K27me3 degree in a concentration-dependent manner in 24 h, had no significant effect on the protein level of EZH1,and significantly increased the expression of EZH2 ubiquitination.
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Cell Line:SU-DHL-2, SU-DHL-4, SU-DHL-6 cells
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Concentration:0-10 µM
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Incubation Time:24 h
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Result:Induced nearly complete cell viability inhibition.
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Cell Line:SU-DHL-6 cells
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Concentration:1, 3, 5 µM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at the G0/G1 phase and a profound sub-G1 population increasein a concentration-dependent manner.
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Cell Line:SU-DHL-6 cells
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Concentration:0-5 µM
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Incubation Time:48 h
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Result:Significantly increased the expression of cleaved caspase-3 and PARP.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude mice (SU-DHL-6 xenograft model)[1]
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Dosage:80 mg/kg
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Administration:I.v.; 6 times for 3 weeks
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Result:Remarkably suppressed the tumor volume and significantly reduced the EZH2 protein and H3K27me3 levels.
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Animal Model:Balb/c nude mice (Jeko-1 xenograft model)[1]
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Dosage:100 mg/kg
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Administration:I.v.; 6 times for 3 weeks
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Result:Shows anti-tumor effects with the significantly reduced the expression of EZH2 protein and H3K27me3 levels.
Chemical Information
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CAS No. 2230914-84-6
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Masse moléculaire 1018.27
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Formule C56H71N7O9S
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SMILES
CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)OCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=CC(C(NCC7=C(C=C(NC7=O)C)C)=O)=C2C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YM281 Related Classifications
HY-145762 Related Classifications
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