2. Apoptosis Epigenetics
  3. Apoptosis Histone Methyltransferase
  4. 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.

For research use only. We do not sell to patients.

YM281 Chemical Structure

YM281 Chemical Structure

CAS No. : 2230914-84-6

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YM281 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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[1].

In Vitro

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.

YM281 Related Antibodies

Western Blot Analysis[1]

Cell Line: SU-DHL-2, 22Rv1 cells
Concentration: 0-6 µM
Incubation Time: 0-48 h
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.

Cell Viability Assay[1]

Cell Line: SU-DHL-2, SU-DHL-4, SU-DHL-6 cells
Concentration: 0-10 µM
Incubation Time: 24 h
Result: Induced nearly complete cell viability inhibition.

Cell Cycle Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 1, 3, 5 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the G0/G1 phase and a profound sub-G1 population increasein a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 0-5 µM
Incubation Time: 48 h
Result: Significantly increased the expression of cleaved caspase-3 and PARP.
In Vivo

YM281 (80, 100 mg/kg; i.v.; 6 times for 3 weeks) shows antitumor effects and significantly reduces the expression of EZH2 protein and H3K27me3 levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c nude mice (SU-DHL-6 xenograft model)[1]
Dosage: 80 mg/kg
Administration: I.v.; 6 times for 3 weeks
Result: Remarkably suppressed the tumor volume and significantly reduced the EZH2 protein and H3K27me3 levels.
Animal Model: Balb/c nude mice (Jeko-1 xenograft model)[1]
Dosage: 100 mg/kg
Administration: I.v.; 6 times for 3 weeks
Result: Shows anti-tumor effects with the significantly reduced the expression of EZH2 protein and H3K27me3 levels.
Molecular Weight

1018.27

Formula

C56H71N7O9S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YM281 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM2812230914-84-6YM 281YM-281ApoptosisHistone MethyltransferaseSU-DHL-6 xenograftlymphomaantitumorapoptosisG0/G1SU-DHL-6 cellscleaved caspase-3ubiquitin-proteasomeInhibitorinhibitorinhibit

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