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

CM-272 

Cat. No.: HY-101925 Purity: 98.13%
Handling Instructions

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor. 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. Anti-tumour Activity.

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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5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 375 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Description

CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor. 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. Anti-tumour Activity[1].

IC50 & Target[1]

G9a

8 nM (IC50)

GLP

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 tumour cells, potentially leading to the induction of cell autonomous immunogenic death in tumour cells[1].

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

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].

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.

1846570-31-7

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)

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
10 mM 0.2089 mL 1.0446 mL 2.0893 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
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Keywords:

CM-272CM272CM 272Histone MethyltransferaseDNA MethyltransferaseApoptosisDNMTsDNA MTasesG9aepigeneticsDNMT1DNMT3ADNMT3BGLPsubstrate-competitiveH3K9me2anti-tumourimmunogenicInhibitorinhibitorinhibit

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CM-272
Cat. No.:
HY-101925
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