Home Epigenetics DNA Methyltransferase inhibitor CM272

CM272

Catalog No.S8812

For research use only.

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

CAS No. 1846570-31-7

Selleck's CM272 has been cited by 1 Publication

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CEMO1 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXS0PEBpenN? MofzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFRV3PNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTBwMkG4{txONg>? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh7MEizNEc,Ojl6OUC4N|A9N2F-
CEMO1 NUDMPVFiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFSzeHk1QCCqcoO= MWTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDDSW1QOSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuNlE5|ryPLh?= M3jZc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUWzPFA6Lz5{OUm1N|gxQTxxYU6=
MV4-11 NV;rOm92T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3nVb|Q5KGi{cx?= NX\2PG1nT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGOgZZN{[XluIFfJOVA:OC5{NkpOwG0v MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl3M{iwPUc,Ojl7NUO4NFk9N2F-
OCI-LY3 NX22[W5{SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MYG0PEBpenN? NWC4O2ZMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPR2kuVFl|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFNiYYPzZZktKEeLNUC9NE41ODoQvF2u M13ueFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEmwPFMxLz5{OUi5NFg{ODxxYU6=
OCI-LY3 MoT4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{L4cVQ5KGi{cx?= MlHGS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gU2NKNUy\MzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVAvPDB7zszNMi=> NXXnOXEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OVM5ODlpPkK5PVU{QDB7PD;hQi=>
OCI-LY10 NILBSnlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXnkbZE2PDhiaILz MlH1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRQ1mtUHkyOCClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUCuOFU2|ryPLh?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh7MEizNEc,Ojl6OUC4N|A9N2F-
OCI-LY10 NWKzd5U5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3;2SlQ5KGi{cx?= M2DZSmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG9EUS2OWUGwJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGOgZZN{[XluIFfJOVA:OC52NUZOwG0v NXLBSI1KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OVM5ODlpPkK5PVU{QDB7PD;hQi=>
LAL-CUN-2 MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH35VGI1QCCqcoO= M2j5dWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGxCVC2FVV6tNkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDHTVUxRTBwNk[0{txONg>? M1ficlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUWzPFA6Lz5{OUm1N|gxQTxxYU6=
THLE2 MWTDfZRwfG:6aXPpeJkh[XO|YYm= NVvBXoFsPzJiaILz NIf5XFZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUEyHMjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygUGM2OD1zLke4{txONg>? MlLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6OUC4N|AoRjJ7OEmwPFMxRC:jPh?=
THLE2 NUHBNlZ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Moj2O|IhcHK| M3HIUWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHRJVEV{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEyFNUC9NU44QM7:TT6= MonTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NUO4NFkoRjJ7OUWzPFA6RC:jPh?=
Click to View More Cell Line Experimental Data
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].

Protocol (from reference)

Cell Research:

[1]
  • 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. "
Animal Research:

[1]
  • Animal Models: 6–8-week-old female BALB/cA−Rag2 γc mice
  • Dosages: 1, 2.5 mg/kg
  • Administration: IV

Solubility (25°C)

In vitro

 DMSO 96 mg/mL
(200.57 mM)
Ethanol 96 mg/mL
(200.57 mM)
Water Insoluble

Chemical Information

Molecular Weight 478.63
Formula

C28H38N4O3

 
CAS No. 1846570-31-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(O1)C2=NC3=CC(=C(C=C3C(=C2)NC4CCN(CC4)C)OC)OCCCN5CCCC5

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