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EPZ020411 hydrochloride

EPZ020411 hydrochloride
EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
Catalog No. T22325Cas No. 2070015-25-5
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Purity:100%
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EPZ020411 hydrochloride

Purity: 100%
Catalog No. T22325Alias EPZ020411 HClCas No. 2070015-25-5

EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
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Pack SizePriceAvailabilityQuantity
1 mg$55In Stock
5 mg$133In Stock
10 mg$226In Stock
25 mg$389In Stock
50 mg$593In Stock
100 mg$848In Stock
1 mL x 10 mM (in DMSO)$148In Stock
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Product Introduction

Bioactivity
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..
AliasEPZ020411 HCl
Chemical Properties
Molecular Weight479.05
FormulaC25H39ClN4O3
Cas No.2070015-25-5
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0875 mL10.4373 mL20.8746 mL104.3732 mL
5 mM0.4175 mL2.0875 mL4.1749 mL20.8746 mL
10 mM0.2087 mL1.0437 mL2.0875 mL10.4373 mL
20 mM0.1044 mL0.5219 mL1.0437 mL5.2187 mL
DMSO
1mg5mg10mg50mg
50 mM0.0417 mL0.2087 mL0.4175 mL2.0875 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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