Home Epigenetics DNA Methyltransferase inhibitor CM272 For research use only.

CM272

CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.

CM272 Chemical Structure

CM272 Chemical Structure

CAS No. 1846570-31-7

Purity & Quality Control

CM272 Related Products

Signaling Pathway

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CEMO1 Antiproliferative assay 48 hrs Antiproliferative activity against human CEMO1 cells after 48 hrs by MTS assay, GI50=0.218μM. 29890830
CEMO1 Growth inhibition assay 48 hrs Growth inhibition of human CEMO1 cells after 48 hrs by MTS assay, GI50=0.218μM. 29953809
MV4-11 Growth inhibition assay 48 hrs Growth inhibition of human MV4-11 cells after 48 hrs by MTS assay, GI50=0.269μM. 29953809
OCI-LY3 Antiproliferative assay 48 hrs Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTS assay, GI50=0.409μM. 29890830
OCI-LY3 Growth inhibition assay 48 hrs Growth inhibition of human OCI-LY3 cells after 48 hrs by MTS assay, GI50=0.409μM. 29953809
OCI-LY10 Antiproliferative assay 48 hrs Antiproliferative activity against human OCI-LY10 cells after 48 hrs by MTS assay, GI50=0.455μM. 29890830
OCI-LY10 Growth inhibition assay 48 hrs Growth inhibition of human OCI-LY10 cells after 48 hrs by MTS assay, GI50=0.455μM. 29953809
LAL-CUN-2 Growth inhibition assay 48 hrs Growth inhibition of human LAL-CUN-2 cells after 48 hrs by MTS assay, GI50=0.664μM. 29953809
THLE2 Cytotoxicity assay 72 hrs Cytotoxicity against human THLE2 cells assessed as reduction in cell viability after 72 hrs by MTS assay, LC50=1.78μM. 29890830
THLE2 Growth inhibition assay 72 hrs Growth inhibition of human THLE2 cells after 72 hrs by MTS assay, LC50=1.78μM. 29953809
Click to View More Cell Line Experimental Data

Biological Activity

Description CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.
Targets
G9a [1]
(Cell-free assay)		 DNMT3A [1]
(Cell-free assay)		 DNMT1 [1]
(Cell-free assay)		 DNMT3B [1]
(Cell-free assay)
8 nM 85 nM 382 nM 1200 nM
In vitro
In vitro

The GI50 for CM-272 after 48 h of treatment in ALL, AML and DLBCL-derived cell lines is in the nM range and is associated with a decrease in global levels of H3K9me2 and 5mC. CM-272 inhibits cell proliferation, blocks cell cycle progression and induces apoptosis in ALL, AML and DLBCL cell lines in a dose-dependent manner. CM-272 induces IFN response and immunogenic cell death.[1].
Cell Research Cell lines ALL, AML, DLBCL, CEMO-1, LAL-CUN-2, MV4-11, OCI-AML-2, OCI-Ly3, OCI-Ly10 cell lines
Concentrations --
Incubation Time 24, 48, 72 and 96h
Method

"100.000 cells of CEMO-1, LAL-CUN-2, MV4-11 and OCI-AML-2 cell lines are cultured at a density of 1x106 cells/mL and treated for 12, 24, 48 and 72 hours with CM-272 at different concentrations (GI25, GI50 and GI75). In the case of OCI-Ly3 and OCI-Ly10, cells are treated with 100, 400 and 1000 nM for 24, 48, 72 and 96h. Cells are washed twice with phosphatebuffered saline (PBS) and resuspended in 1X Binding Buffer at a concentration of 1x106 cells/mL. 1 µL of FITC Annexin V antibody and 2 µL of propidium iodide are added and incubated for 15 min at RT in the dark. Finally, 400 µL of 1X Binding Buffer are added to each tube and analyzed by flow cytometry within 1 h. "
In Vivo
In vivo

CM272 therapy induces a statistically significant increase in overall survival (OS) in mice in comparison with control animals. Global H3K9me2 and 5mC levels are reduced in leukaemic cells obtained from mice engrafted with ALL-derived CEMO-1 cells after 1 week of treatment and no significant weight loss is observed in treated animals. CM272 shows dose-dependent efficacy and a dose of 2.5 mg/kg of CM272 is adequate to demonstrate the positive anti-tumour efficacy in mice engrafted with ALL-derived CEMO-1 cells.[1].
Animal Research Animal Models 6–8-week-old female BALB/cA−Rag2 γc mice
Dosages 1, 2.5 mg/kg
Administration IV

Chemical Information & Solubility

Molecular Weight 478.63 Formula

C28H38N4O3

 
CAS No. 1846570-31-7 SDF --
Smiles CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (200.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 96 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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