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EPZ015666 (GSK3235025)
EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
EPZ015666 (GSK3235025) Chemical Structure
CAS No. 1616391-65-1
Purity & Quality Control
Batch:
Purity: >97%
97
EPZ015666 (GSK3235025) Related Products
Signaling Pathway
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| MDA-MB-468 | Function assay | 48 h | inhibits PRMT5 activity | 30957988 | ||
| HCC1954 | Cell viability assay | IC50=0.8 μM | 30957988 | |||
| MDA-MB-453 | Cell viability assay | IC50=1 μM | 30957988 | |||
| HCC38 | Cell viability assay | IC50=2.2 μM | 30957988 | |||
| MDA-MB-468 | Cell viability assay | IC50=2.2 μM | 30957988 | |||
| MCF7 | Cell viability assay | IC50=2.6 μM | 30957988 | |||
| SKBR3 | Cell viability assay | IC50=3.9 μM | 30957988 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [3H]-SAM by Topcount method, IC50=0.022μM | 29628326 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [4H]-SAM by Topcount method, IC50=0.022μM | 29628326 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [5H]-SAM by Topcount method, IC50=0.022μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [6H]-SAM by Topcount method, IC50=0.022μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [7H]-SAM by Topcount method, IC50=0.047μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [8H]-SAM by Topcount method, IC50=0.047μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [9H]-SAM by Topcount method, IC50=0.047μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [10H]-SAM by Topcount method, IC50=0.047μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [11H]-SAM by Topcount method, IC50=0.047μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [12H]-SAM by Topcount method, IC50=0.047μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [13H]-SAM by Topcount method, IC50=0.096μM | 29870258 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [14H]-SAM by Topcount method, GI50=0.106μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [15H]-SAM by Topcount method, GI50=0.106μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [16H]-SAM by Topcount method, GI50=0.212μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [17H]-SAM by Topcount method, GI50=0.212μM | 30605830 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [18H]-SAM by Topcount method, IC50=0.45μM | 29870258 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [19H]-SAM by Topcount method, IC50=0.96μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [20H]-SAM by Topcount method, IC50=1.1μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [21H]-SAM by Topcount method, IC50=1.8μM | 30366617 | |||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [22H]-SAM by Topcount method, IC50=2.6μM | 30366617 | |||
| Click to View More Cell Line Experimental Data | ||||||
Biological Activity
| Description | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. | ||
|---|---|---|---|
| Targets |
|
| In vitro | ||||
| In vitro | EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1] |
|||
|---|---|---|---|---|
| Cell Research | Cell lines | MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) | ||
| Concentrations | 5 μM | |||
| Incubation Time | 12 days | |||
| Method | -- |
|||
| Experimental Result Images | Methods | Biomarkers | Images | PMID |
| Western blot | H4R3me2s PRMT5 / H3R8me2s |
|
28945229 | |
| Immunofluorescence | IKKβ |
|
29158558 | |
| Growth inhibition assay | Cell viability |
|
30957988 | |
| In Vivo | ||
| In vivo | EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1] |
|
|---|---|---|
| Animal Research | Animal Models | MCL (Z-138, and Maver-1) xenograft models |
| Dosages | 200 mg/kg BID | |
| Administration | p.o. | |
Chemical Information & Solubility
| Molecular Weight | 383.44 | Formula | C20H25N5O3 |
| CAS No. | 1616391-65-1 | SDF | Download EPZ015666 (GSK3235025) SDF |
| Smiles | C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O | ||
| Storage (From the date of receipt) | |||
|
In vitro |
DMSO : 77 mg/mL ( (200.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Ethanol : 26 mg/mL Water : Insoluble |
Molecular Weight Calculator |
|
In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
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Preparing Stock Solutions
Molarity Calculator
In vivo Formulation Calculator (Clear solution)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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