EPZ015666 (GSK3235025)

For research use only.

Catalog No.S7748

12 publications

EPZ015666 (GSK3235025) Chemical Structure

CAS No. 1616391-65-1

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 12 publications

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

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

Proc Natl Acad Sci U S A, 2020, 117(45):28068-28079

PubMed: 33097661 ( click the link to review the publication )

Signal Transduct Target Ther, 2020, 5(1):197

PubMed: 32994405 ( 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 )

Oxid Med Cell Longev, 2019, 2019:2345658

PubMed: 31885778 ( click the link to review the publication )

BMC Cancer, 2019, 19(1):1056

PubMed: 31694585 ( 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 )

Sci Signal, 2016, 9(443):rs9

PubMed: 27577262 ( 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	M3LVTWZ2dmO2aX;uJIF{e2G7	M1vNS\|Q5KGh?	M{nQO4lvcGmkaYTzJHBTVVR3IHHjeIl3cXS7	MVmzNFk2Pzl6OB?=
HCC1954	MojDR4VtdCC4aXHibYxqfHliYYPzZZk>		NFrsN2dKSzVyPUCuPEDPxE1?	MV[zNFk2Pzl6OB?=
MDA-MB-453	NIq2ZlZE\WyuII\pZYJqdGm2eTDhd5NigQ>?		NFzNOYlKSzVyPUGg{txO	NEfLUpY{ODl3N{m4PC=>
HCC38	MmXTR4VtdCC4aXHibYxqfHliYYPzZZk>		M2TBW2lEPTB;Mj6yJO69VQ>?	MnLxN\|A6PTd7OEi=
MDA-MB-468	NIe2V4pE\WyuII\pZYJqdGm2eTDhd5NigQ>?		NInoT3lKSzVyPUKuNkDPxE1?	MUOzNFk2Pzl6OB?=
MCF7	MmDCR4VtdCC4aXHibYxqfHliYYPzZZk>		NI\Ze2tKSzVyPUKuOkDPxE1?	MUizNFk2Pzl6OB?=
SKBR3	NYCyWopIS2WubDD2bYFjcWyrdImgZZN{[Xl?		MmDCTWM2OD1\|Lkmg{txO	MkTZN\|A6PTd7OEi=

... 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 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)
	Water	Insoluble
	Ethanol	'48 mg/mL warmed
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 2 years-80°C in solvent
Synonyms
Smiles	C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

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.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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.

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)