EPZ015666(GSK3235025)

Name: EPZ015666(GSK3235025)
Brand: Selleck Chemicals
SKU: S7748
Rating: 5 (7 reviews)

For research use only. Not for use in humans.

Catalog No.S7748 Synonyms: GSK3235025

7 publications

EPZ015666(GSK3235025) Chemical Structure

Molecular Weight(MW): 383.44

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

Selleck's EPZ015666(GSK3235025) has been cited by 7 publications

Cancer Cell, 2017, 32(4):411-426

PubMed: 28966034 ( click the link to review the publication )

Theranostics, 2019, 9(9):2606-2617

PubMed: 31131056 ( click the link to review the publication )

EBioMedicine, 2019, 44:98-111

PubMed: 31101597 ( click the link to review the publication )

Front Immunol, 2019, 10:174

PubMed: 30800128 ( click the link to review the publication )

Osteoarthritis Cartilage, 2019, 27(6):932-944

PubMed: 30858101 ( click the link to review the publication )

J Cell Mol Med, 2017, 21(4):781-790

PubMed: 27860244 ( click the link to review the publication )

Cell Signal, 2017, 34:55-65

PubMed: 28302565 ( click the link to review the publication )

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 K_i 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	Incubation Time	Activity Description	PMID
MDA-MB-468	MUDGeY5kfGmxbjDhd5NigQ>?	NFz4fYI1QCCq	NHnoeYZqdmirYnn0d{BRWk2WNTDhZ5Rqfmm2eR?=	MljFN\|A6PTd7OEi=
HCC1954	MlLvR4VtdCC4aXHibYxqfHliYYPzZZk>		MUnJR\|UxRTBwODFOwG0>	NF;Qd4k{ODl3N{m4PC=>
MDA-MB-453	M1\BTWNmdGxidnnhZoltcXS7IHHzd4F6		NHmzeXVKSzVyPUGg{txO	NFv3VHc{ODl3N{m4PC=>
HCC38	MVzD[YxtKH[rYXLpcIl1gSCjc4PhfS=>		MUfJR\|UxRTJwMjFOwG0>	NIXkNG8{ODl3N{m4PC=>
MDA-MB-468	NUL4e2dYS2WubDD2bYFjcWyrdImgZZN{[Xl?		MVXJR\|UxRTJwMjFOwG0>	NUSxWoFDOzB7NUe5PFg>
MCF7	MV7D[YxtKH[rYXLpcIl1gSCjc4PhfS=>		Mn:xTWM2OD1{Lk[g{txO	M1LTN\|MxQTV5OUi4
SKBR3	NX:3N4tWS2WubDD2bYFjcWyrdImgZZN{[Xl?		NYWwc5dTUUN3ME2zMlkh\|ryP	M4fpT\|MxQTV5OUi4

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	H4R3me2s; PubMed: 28945229 Oncogene 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 Cancer Med 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 Leukemia 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 Cancer Med 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]	- Collapse 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]	- Collapse 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)

References

[1] Penebre et al. Epizyme, Inc.

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 Download EPZ015666(GSK3235025) SDF

Molecular Weight	383.44
Formula	C₂₀H₂₅N₅O₃
CAS No.	1616391-65-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	GSK3235025
Smiles	OC(CNC(=O)C1=CC(=NC=N1)NC2COC2)CN3CCC4=C(C3)C=CC=C4

Bio Calculators

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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

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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.

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EPZ015666(GSK3235025)