1. Epigenetics
  2. Histone Methyltransferase
  3. DM-01

DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.

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

DM-01 Chemical Structure

DM-01 Chemical Structure

CAS No. : 2355280-00-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 420 In-stock
25 mg USD 840 In-stock
50 mg USD 1250 In-stock
100 mg USD 1800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors[1].

IC50 & Target[1]

EZH2

 

In Vitro

Knockdown EZH2 in A549 cells results in the decrease of cell sensitivity to DM-01 at 50 and 100 μM concentrations. DM-01 also shows comparable inhibitory activity for K562 cells with an IC50 value of 58.706 μΜ[1].
DM-01 (5 and 10 μM; 24 hours) strongly inhibits the activity of EZH2 and results in abolished H3K27me expression in K562 cells[1].
DM-01 (5 and 10 μM) also increases the transcription expression of DIRAS3 in a dose dependent manner, a tumor suppressor in downstream of EZH2[1].

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

Cell Viability Assay[1]

Cell Line: A549 sh-EV and A549 sh-EZH2 cells
Concentration: 1, 5, 10, 50, 100 μM
Incubation Time: 48 hours
Result: The IC50s of 72.748 and 269.7 μΜ for A549 sh-EV and A549 sh-EZH2 cells, respectively.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 5, 10 μM
Incubation Time: 24 hours
Result: Inhibited the activity of EZH2 and resulted in abolished H3K27me expression.
Molecular Weight

431.45

Formula

C23H24F3N3O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)N(CC2=CC=C(C(F)(F)F)C=C2)C=C1C)NCC3=C(C)C=C(C)NC3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (115.89 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 2.3178 mL 11.5888 mL 23.1777 mL
5 mM 0.4636 mL 2.3178 mL 4.6355 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (stored under nitrogen). 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 2.3178 mL 11.5888 mL 23.1777 mL 57.9441 mL
5 mM 0.4636 mL 2.3178 mL 4.6355 mL 11.5888 mL
10 mM 0.2318 mL 1.1589 mL 2.3178 mL 5.7944 mL
15 mM 0.1545 mL 0.7726 mL 1.5452 mL 3.8629 mL
20 mM 0.1159 mL 0.5794 mL 1.1589 mL 2.8972 mL
25 mM 0.0927 mL 0.4636 mL 0.9271 mL 2.3178 mL
30 mM 0.0773 mL 0.3863 mL 0.7726 mL 1.9315 mL
40 mM 0.0579 mL 0.2897 mL 0.5794 mL 1.4486 mL
50 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1589 mL
60 mM 0.0386 mL 0.1931 mL 0.3863 mL 0.9657 mL
80 mM 0.0290 mL 0.1449 mL 0.2897 mL 0.7243 mL
100 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5794 mL
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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.

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DM-01
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