2. Epigenetics Apoptosis
  3. Histone Methyltransferase DNA Methyltransferase Apoptosis
  4. CM-272

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.

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

CM-272 Chemical Structure

CM-272 Chemical Structure

CAS No. : 1846570-31-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 211 In-stock
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10 mM * 1 mL in DMSO USD 211 In-stock
Solid
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Customer Review

Based on 1 publication(s) in Google Scholar

CM-272 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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DNA Methyltransferase DNMT1 DNMT3 MGMT

  • Biological Activity

  • Purity & Documentation

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Description

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death[1].

IC50 & Target[1]

G9a

8 nM (IC50)

EHMT1/GLP/KMT1D

2 nM (IC50)

DNMT1

382 nM (IC50)

DNMT3A

85 nM (IC50)

DNMT3B

1200 nM (IC50)

In Vitro

CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment inhibits cell proliferation in a dose- and time-dependent manner[1].
CM-272 (100-1000 nM; 24 hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression[1].
CM-272 (100-1000 nM; 12-72 hours; CEMO-1, MV4-11, and OCI-Ly10 cell lines) treatment induces apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner[1].
CM-272 after 48 h of treatment CEMO-1 acute lymphoblastic leukaemia (ALL) cell line, MV4-11 acute myeloid leukaemia (AML) cell line, and OCI-Ly10 diffuse large B-cell lymphoma (DLBCL) cell line, the GI50 values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC[1].
The therapeutic activity of CM-272 relies on the early activation of the type I IFN response in tumor cells, potentially leading to the induction of cell-autonomous immunogenic death in tumor cells[1].

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

CM-272 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time: 12 hours, 24 hours, 48 hours and 72 hours
Result: Inhibited cell proliferation in a dose- and time-dependent manner.

Cell Cycle Analysis[1]

Cell Line: CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time: 24 hours
Result: Blocked cell cycle progression.

Apoptosis Analysis[1]

Cell Line: CEMO-1, MV4-11 and OCI-Ly10 cell lines
Concentration: 125 nM, 250 nM, 500 nM (CEMO-1 cells); 135 nM, 270 nM, 540 nM (MV4-11 cells); 100 nM, 400 nM, 1000 nM (OCI-Ly10 cells)
Incubation Time: 12 hours, 24 hours, 48 hours and 72 hours
Result: Induced apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner.
In Vivo

CM-272 (2.5 mg/kg; intravenous injection; daily; for 28 days; female Rag2 / γc / mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models[1].

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

Animal Model: Female BALB/Ca-Rag2−/−γc−/− mice (6–8-week-old) with CEMO-1 cells[1]
Dosage: 2.5 mg/kg
Administration: Intravenous injection; daily; for 28 days
Result: Induced a statistically significant increase in overall survival (OS) in mice.
Molecular Weight

478.63

Formula

C28H38N4O3
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

CN(CC1)CCC1NC2=CC(C3=CC=C(C)O3)=NC4=CC(OCCCN5CCCC5)=C(OC)C=C42
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 (261.16 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 2.0893 mL 10.4465 mL 20.8930 mL
5 mM 0.4179 mL 2.0893 mL 4.1786 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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).
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

Purity: 99.27%

COA (248 KB) HNMR (293 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
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 2.0893 mL 10.4465 mL 20.8930 mL 52.2324 mL
5 mM 0.4179 mL 2.0893 mL 4.1786 mL 10.4465 mL
10 mM 0.2089 mL 1.0446 mL 2.0893 mL 5.2232 mL
15 mM 0.1393 mL 0.6964 mL 1.3929 mL 3.4822 mL
20 mM 0.1045 mL 0.5223 mL 1.0446 mL 2.6116 mL
25 mM 0.0836 mL 0.4179 mL 0.8357 mL 2.0893 mL
30 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7411 mL
40 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
50 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0446 mL
60 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8705 mL
80 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
100 mM 0.0209 mL 0.1045 mL 0.2089 mL 0.5223 mL
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CM-272 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:

CM-2721846570-31-7CM272CM 272Histone MethyltransferaseDNA MethyltransferaseApoptosisDNMTsDNA MTasesG9aepigeneticsDNMT1DNMT3ADNMT3BGLPsubstrate-competitiveH3K9me2anti-tumourimmunogenicInhibitorinhibitorinhibit

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