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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Based on 1 publication(s) in Google Scholar

YM458 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 NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(NCCCCCOC4=CC=C(C5=CC(N(C6CCOCC6)CC)=C(C(C(NCC7=C(C=C(NC7=O)C)C)=O)=C5)C)C=C4)=O)C8=NN=C(C)N28
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (130.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0443 mL 5.2213 mL 10.4426 mL
5 mM 0.2089 mL 1.0443 mL 2.0885 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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 1.0443 mL 5.2213 mL 10.4426 mL 26.1064 mL
5 mM 0.2089 mL 1.0443 mL 2.0885 mL 5.2213 mL
10 mM 0.1044 mL 0.5221 mL 1.0443 mL 2.6106 mL
15 mM 0.0696 mL 0.3481 mL 0.6962 mL 1.7404 mL
20 mM 0.0522 mL 0.2611 mL 0.5221 mL 1.3053 mL
25 mM 0.0418 mL 0.2089 mL 0.4177 mL 1.0443 mL
30 mM 0.0348 mL 0.1740 mL 0.3481 mL 0.8702 mL
40 mM 0.0261 mL 0.1305 mL 0.2611 mL 0.6527 mL
50 mM 0.0209 mL 0.1044 mL 0.2089 mL 0.5221 mL
60 mM 0.0174 mL 0.0870 mL 0.1740 mL 0.4351 mL
80 mM 0.0131 mL 0.0653 mL 0.1305 mL 0.3263 mL
100 mM 0.0104 mL 0.0522 mL 0.1044 mL 0.2611 mL
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YM458 Related Classifications

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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