| Name | EPZ020411 hydrochloride |
| Description | EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM. |
| Cell Research | Cell lines: A375 cells. Concentrations: 0-20 μM. Incubation Time: 48 h. Method: A375 (CRL-1619) cells are cultured in DMEM with 10% (vol/vol) FBS. PRMT6 is cloned into EcoRI and BamHI sites of a pcDNA4 HisMAX_A plasmid. According to procedures recommended by the manufacturer, transfection of his-tagged PRMT6 or vector control is carried out using Lipofectamine LTX and Plus reagent . Cells are seeded at 200,000 cells/well in 6-well plates. The second day, the cells are concurrently transfected and treated with compound in 0.25% DMSO. Cells are incubated in the presence compound at 20 μM and collected after 48 hours treatment. |
| Animal Research | Animal Models: SD rats. Dosages: 1 mg/kg. Administration: i.v.. |
| In vitro | Treatment with EPZ020411 results in a dose-dependent decrease in H3R2 methylation in A375 human melanoma cells exogenously overexpressing PRMT6(IC50=0.637±0.241 μM). EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including PRMT3, PRMT4, PRMT5, and PRMT7 in biochemical assays. The compound shows poor permeability in the parallel artificial membrane permeation assay[1]. |
| In vivo | EPZ020411 shows good bioavailability following subcutaneous dosing in rats. Male Sprague-Dawley rats administered EPZ020411 at a single dose of 1 mg/kg by i.v. bolus show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. A good bioavailability of 65.6 ± 4.3% is observed following 5 mg/kg s.c. dosing, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 for more than 12 h[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.17 mM), Sonication is recommended.
H2O : 18 mg/mL (37.57 mM), Sonication and heating to 60℃ are recommended.
DMSO : 45 mg/mL (93.94 mM), Sonication is recommended.
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| Keywords | PRMT8 | PRMT6 | PRMT1 | HistoneMethyltransferase | Histone Methyltransferase | EPZ-020411 hydrochloride | EPZ020411 Hydrochloride | EPZ 020411 Hydrochloride |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Compound Library | High-Efficiency Gene Editing Small Molecule Library |
United States
