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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $55 | In Stock | |
5 mg | $133 | In Stock | |
10 mg | $226 | In Stock | |
25 mg | $389 | In Stock | |
50 mg | $593 | In Stock | |
100 mg | $848 | In Stock | |
1 mL x 10 mM (in DMSO) | $148 | In Stock |
Description | EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM. |
Targets&IC50 | PRMT6:10 nM, PRMT1:119 nM, PRMT8:223 nM |
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]. |
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.. |
Alias | EPZ020411 HCl |
Molecular Weight | 479.05 |
Formula | C25H39ClN4O3 |
Cas No. | 2070015-25-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 18.0 mg/mL (37.6 mM), Sonication and heating to 60℃ are recommended. DMSO: 45.0 mg/mL (93.9 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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