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

EPZ015666 (GSK3235025) Chemical Structure

CAS: 1616391-65-1

Selleck's EPZ015666 (GSK3235025) has been cited by 27 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: >97%
97

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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
PRMT5 [1]
(Cell-free assay)
5 nM(Ki)
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

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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
Batch:

DMSO : 77 mg/mL ( (200.81 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 26 mg/mL

Water : Insoluble


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In vivo
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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.

Handling Instructions

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