2140164-84-5
Chemical Structure
EZM8266
- CAS No.: 2140164-84-5
- Formula:C19H27N5O3
- Molecular Weight:373.45
InChIKey: KUENQALMXHZZBJ-OAHLLOKOSA-N
SMILES: CNC1=NC(NC2=CC(OC[C@@H](CN3CCC3)O)=C(C=C2)OC)=NC(C)=C1
Biological Activity: EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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EZM8266 | 98.24% | EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma. | ||||||||||||||||||||
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- [1]. Adan-Villaescusa E, et al. Histone methyl-transferase G9a inhibition boosts the efficacy of immune checkpoint inhibitors in experimental hepatocellular carcinoma. Cell Rep Med. 2026;7(4):102717. [Content Brief]
- [2]. Campbell JE, et al. Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof. United States, WO2019079540 A. 2017-10-18.
Keywords
