EPZ015666(GSK3235025)

Catalog No.S7748 Synonyms: GSK3235025

EPZ015666(GSK3235025) Chemical Structure

Molecular Weight(MW): 383.44

EPZ015666(GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.

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Cited by 4 Publications

1 Customer Review

  • (B) Effect of EPZ015666 on nuclear translocation of p65. Middle panel showed a representative photo of IF staining of p65 localization (green). Nuclei were stained with DAPI.

    J Cell Mol Med, 2016, 1-10.. EPZ015666(GSK3235025) purchased from Selleck.

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-468 MUjGeY5kfGmxbjDhd5NigQ>? MmPIOFghcA>? NFLuTZVqdmirYnn0d{BRWk2WNTDhZ5Rqfmm2eR?= NXWwSINvOzB7NUe5PFg>
HCC1954 NWrle2V1S2WubDD2bYFjcWyrdImgZZN{[Xl? NEm0TolKSzVyPUCuPEDPxE1? Mm\rN|A6PTd7OEi=
MDA-MB-453 M{XnV2NmdGxidnnhZoltcXS7IHHzd4F6 NWmzRmQ{UUN3ME2xJO69VQ>? MlvoN|A6PTd7OEi=
HCC38 NUHZS4ttS2WubDD2bYFjcWyrdImgZZN{[Xl? MYTJR|UxRTJwMjFOwG0> NXHwb|dJOzB7NUe5PFg>
MDA-MB-468 MkP5R4VtdCC4aXHibYxqfHliYYPzZZk> MmH4TWM2OD1{LkKg{txO MYqzNFk2Pzl6OB?=
MCF7 M4PROGNmdGxidnnhZoltcXS7IHHzd4F6 NIjkPWxKSzVyPUKuOkDPxE1? M{K2XlMxQTV5OUi4
SKBR3 NGfYN2pE\WyuII\pZYJqdGm2eTDhd5NigQ>? NW[2bmNTUUN3ME2zMlkh|ryP M2nvS|MxQTV5OUi4

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
H4R3me2s; 

PubMed: 28945229     


U937 (CALM-AF10), NB4 (PML-RARα), and MonoMac6 (MLL-AF9) cell lines were dosed with EPZ015666 at indicated concentrations. H4R3me2s is shown at Day 4 for the 10, 3, 1, and 0μM doses.

PRMT5 / H3R8me2s ; 

PubMed: 30957988     


EPZ015666 inhibits PRMT5 activity. MDA‐MB‐468 cells were treated with the indicated concentration of the PRMT5 inhibitor EPZ015666 or with vehicle (DMSO). PRMT5 activity was assessed 48 h later by Western‐Blot analysis using antibodies that recognize symmetric dimethyl‐arginine on histones H3 (H3R8me2s) and H4 (H4R3me2s). PRMT5 expression was verified. Actin was used as a loading control. Images are from a single experiment representative of three independent experiments.

28945229 30957988
Immunofluorescence
IKKβ; 

PubMed: 29158558     


H929 were treated with EPZ015666. After treatment, samples dual stained with Cyto-ID Green dye and IKKβ antibody were analyzed by fluorescence microscopy. Arrows indicate colocalization of IKKβ in the autophagosome.

29158558
Growth inhibition assay
Cell viability; 

PubMed: 30957988     


Treatment of breast cell lines with PRMT5 inhibitor EPZ015666 identifies a group of sensitive cell lines and a group of resistant cell lines. Cell viability was determined by MTT assay after four doubling times. Results are expressed as the percentage of cell growth relative to vehicle‐treated cells. The mean of at least three independent experiments for each cell line is presented. Breast cancer subtypes are indicated as follows: green (ER+), blue (ER‐/HER2+), red (ER‐/PR‐/HER2‐). The non‐tumorigenic breast cells, MCF‐10A and MCF‐12A, are in black.

30957988
In vivo EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1]

Protocol

Cell Research:

[1]
+ Expand
  • Cell lines: MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1)
  • Concentrations: 5 μM
  • Incubation Time: 12 days
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]
+ Expand
  • Animal Models: MCL (Z-138, and Maver-1) xenograft models
  • Formulation: 0.5 % MC
  • Dosages: 200 mg/kg BID
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL warmed (156.47 mM)
Ethanol 48 mg/mL warmed (125.18 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.44
Formula

C20H25N5O3
CAS No. 1616391-65-1
Storage powder
in solvent
Synonyms GSK3235025

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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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    I want to use this compound for injection, how to reconstitute it?

  • Answer:

    S7748, EPZ015666 is a clear solution in 2% DMSO+30% PEG300+68% water and it can be used for tail vein injection.

selleck catalog

Histone Methyltransferase Signaling Pathway Map
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID