YM1240
YM1240 is an orally active dual EZH2/HDAC inhibitor with human EZH2 IC50 0.342 μM and human HDAC IC50 0.12 μM. YM1240 inhibits EZH2 pathway to reduce H3K27me3 levels, inhibits HDAC pathway to increase H3K9ac and H4ac levels. YM1240 suppresses proliferation, induces apoptosis, induces cell cycle arrest in lymphoma cells. YM1240 exhibits antitumor efficacy in lymphoma xenograft models. YM1240 can be used for the research of lymphoma.
For research use only. We do not sell to patients.
- Formula: C29H30N4O4
- Molecular Weight:498.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
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HDAC 0.12 μM (IC50) |
EZH2 0.342 μM (IC50) |
YM1240 (compound D19) (0.3-0.6 μM; 60 min) potently inhibits the activity of purified EZH2 enzyme, with an IC50 of 0.342 μM; it also potently inhibits HDAC enzyme activity in HeLa nuclear extracts, with an IC50 of 0.12 μM[1].
YM1240 (60 min) is a potent and selective inhibitor of HDAC1 and HDAC6, with IC50 values of 0.066 μM and 0.01 μM, respectively. It exhibits negligible activity against HDAC4 and only weak activity against HDAC8[1].
YM1240 (0.01-10 μM; 6 days) potently inhibits the proliferation of Jeko-1, NAMALWA, RAJI, DAUDI, JVM-2 and Mino lymphoma cell lines, with GC50 values ranging from 0.20 μM to 0.92 μM; it also potently inhibits the proliferation of SU-DHL-2 lymphoma cells, with a GC50 of 0.26 μM[1].
YM1240 (1-4 μM; 24 h) inhibits EZH2 activity (reduces H3K27me3 levels) and HDAC activity (increases H3K9ac and H4ac levels) in Jeko-1 and SU-DHL-2 lymphoma cells in a dose-dependent manner[1].
YM1240 (1-2 μM; 72 h) induces apoptosis in Jeko-1 and SU-DHL-2 lymphoma cells in a dose-dependent manner, as evidenced by increased Annexin V-positive cells and elevated levels of activated caspase 3/7 and activated PARP[1].
YM1240 (1-2 μM; 48 h) induces G0/G1 cell cycle arrest in Jeko-1 and SU-DHL-2 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:Jeko-1, NAMALWA, RAJI, DAUDI, JVM-2, and Mino lymphoma cell, SU-DHL-2 lymphoma cell
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:6 days
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Result:Inhibited proliferation of Jeko-1, NAMALWA, RAJI, DAUDI, JVM-2, and Mino lymphoma cell lines, with GC50 values ranging from 0.20 μM to 0.92 μM.
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Cell Line:Jeko-1 and SU-DHL-2 lymphoma cell
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Concentration:1, 2, 4 μM
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Incubation Time:24 h
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Result:Inhibited EZH2 activity (reducing H3K27me3) and HDAC activity (increasing H3K9ac and H4ac) in Jeko-1 and SU-DHL-2 lymphoma cells.
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Cell Line:Jeko-1 and SU-DHL-2 lymphoma cell
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Concentration:1, 2 μM
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Incubation Time:72 h
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Result:Induced apoptosis in Jeko-1 and SU-DHL-2 lymphoma cells after 72 h of treatment.
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Cell Line:Jeko-1 and SU-DHL-2 lymphoma cell
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Concentration:1, 2 μM
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Incubation Time:48 h
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Result:Induced G0/G1 phase cell cycle arrest.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 498.57
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Formula C29H30N4O4
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SMILES
O=C(C1=CC(C2=CC=CC(/C=C/C(NO)=O)=C2)=CC3=C1C=CN3C(C)C)NCC4=C(C)C=C(C)NC4=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)