2095432-47-4
Chemical Structure
EPZ020411 dihydrochloride
- CAS No.: 2095432-47-4
- Formula:C25H40Cl2N4O3
- Molecular Weight:515.52
IUPAC Name: N1,N2-dimethyl-N1-((3-(4-((1r,3r)-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine hydrochloride
InChIKey: QCHZLIPYCYHFLI-PZPNUJOOSA-N
SMILES: CNCCN(C)CC1=CNN=C1C2=CC=C(C=C2)O[C@H]3C[C@@H](C3)OCCC4CCOCC4.Cl.Cl
Biological Activity: EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma[1][2][3][4][5].
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EPZ020411 dihydrochloride | EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma. | |||||||||||||||||||||
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- [1]. Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound. ACS Med Chem Lett. 2015;6(6):655-659. Published 2015 Apr 6. [Content Brief]
- [2]. Hua T, et al. PRMT6 deficiency or inhibition alleviates neuropathic pain by decreasing glycolysis and inflammation in microglia. Brain Behav Immun. 2024;118:101-114. [Content Brief]
- [3]. Duan J, et al. Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer. J Immunother Cancer. 2025;13(3):e010639. Published 2025 Mar 13. [Content Brief]
- [4]. He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020;10(1):133-150. Published 2020 Jan 1. [Content Brief]
- [5]. Wang J, et al. PRMT6 facilitates EZH2 protein stability by inhibiting TRAF6-mediated ubiquitination degradation to promote glioblastoma cell invasion and migration. Cell Death Dis. 2024;15(7):524. Published 2024 Jul 23. [Content Brief]
Keywords
