2. Epigenetics Apoptosis
  3. Histone Methyltransferase Epigenetic Reader Domain Apoptosis
  4. YM458

YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.

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

YM458 Chemical Structure

YM458 Chemical Structure

CAS No. : 2770108-93-3

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YM458 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

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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

YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer[1].

IC50 & Target[1]

EZH2

 

EZH2

490 nM (IC50)

BRD4

34 nM (IC50)

In Vitro

YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC50 of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1[1].
YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM[1].
YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner[1].

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

YM458 Related Antibodies

Western Blot Analysis

Cell Line: AsPC-1[1]
Concentration: 1 μM
Incubation Time: 72 hours
Result: Decreased the degree of H3K27me3 and c-Myc significantly.

Cell Proliferation Assay

Cell Line: AsPC-1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO[1]
Concentration: 0-30 μM
Incubation Time: 4 or 6 days
Result: Inhibited cell proliferation on a broad range of solid cancer cells, and significantly suppressed proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM.
In Vivo

YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells[1].
Pharmacokinetic Parameters of YM458 in Female BALB/c mice[1].

IP (80 mg/kg) PO (80 mg/kg)
t1/2 (h) 3.81 4.16
Tmax (h) 1 1
Cmax (ng/mL) 27126.3 4383.6
AUC0-24 (ng/mL·h) 273220.1 13509.1
CL (mL/min/kg) 4.88
F (%) 4.94

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

Animal Model: BALB/c nude mice (injected with A549 or AsPC-1)[1]
Dosage: 60 mg/kg
Administration: IP; every other day, for 38 days
Result: Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.
Molecular Weight

957.62

Formula

C53H61ClN8O5S
CAS No.
SMILES

CC1=C(C2=C(S1)N3C([C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NCCCCCOC5=CC=C(C6=CC(N(CC)C7CCOCC7)=C(C(C(NCC8=C(C=C(NC8=O)C)C)=O)=C6)C)C=C5)=O)=NN=C3C)C
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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YM458 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:

YM4582770108-93-3YM 458YM-458Histone MethyltransferaseEpigenetic Reader DomainApoptosisAnticancerCell proliferationColony formationCell cycle arrestSolid cancer cellsA549Inhibitorinhibitorinhibit

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