| Identification | Back Directory | [Name]
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride | [CAS]
2070015-25-5 | [Synonyms]
EPZ020411 hydrochloride
(EPZ-020411 hydrochloride
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride | [Molecular Formula]
C25H39ClN4O3 | [MDL Number]
MFCD29924736 | [MOL File]
2070015-25-5.mol | [Molecular Weight]
479.055 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at 4°C, stored under nitrogen | [solubility ]
DMSO: 50 mg/mL (104.37 mM); Water: ≥ 41 mg/mL (85.58 mM) | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer[1][2]. | [Biological Activity]
EPZ020411 hydrochloride is a potent and selective small molecule inhibitor of PRMT6 with IC50 of 10 nM. | [in vitro]
EPZ020411 hydrochloride dose-dependently reduced H3R2 methylation in human melanoma A375 cells overexpressing PRMT6 (IC50=0.637±0.241 μM). In biochemical assays, the selectivity of EPZ020411 to PRMT6/8/1 was more than 100-fold higher than that of other histone methyltransferases (including 4 arginine methyltransferases PRMT3, PRMT4, PRMT5, PRMT7). In the parallel artificial membrane permeation test, EPZ020411 has poor permeability. | [in vivo]
EPZ020411 hydrochloride has good bioavailability in rats by subcutaneous injection and is a suitable compound for in vivo studies. After a single intravenous injection of 1 mg/kg EPZ020411 hydrochloride into male Sprague-Dawley rats, its in vivo clearance (CL) was 19.7 ± 1.0 mL/min/kg and its volume of distribution at steady state (Vss) was 11.1 ± 1.6 L/kg, the average half-life was 8.54±1.43 h. Subcutaneous injection of 5 mg/kg has good bioavailability of 65.6 ± 4.3%, and the free concentration of EPZ020411 in the blood is higher than the biochemical IC50 value of PRMT6 for more than 12 hours. | [target]
| Target | Value | PRMT6
(Cell-free assay) | 10 nM | PRMT1
(Cell-free assay) | 119 nM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> PRMT8
(Cell-free assay) 223 nM |
| [IC 50]
PRMT6: 0.01 μM (IC50); PRMT1: 0.119 μM (IC50); PRMT8: 0.223 μM (IC50) | [References]
[1] Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659. DOI:10.1021/acsmedchemlett.5b00071
[2] 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 Jan 1;10(1):133-150. DOI:10.7150/thno.37362 |
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| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|