Home Epigenetics Histone Methyltransferase inhibitor - PRMT inhibitor Pemrametostat (GSK3326595) For research use only.

Pemrametostat (GSK3326595)

Synonyms: EPZ015938

Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.

Pemrametostat (GSK3326595) Chemical Structure

Pemrametostat (GSK3326595) Chemical Structure

CAS No. 1616392-22-3

Purity & Quality Control

Products often used together with Pemrametostat (GSK3326595)

Santacruzamate A (CAY10683)

Pemrametostat and Santacruzamate A treatments rescue the ZEB2-mediated E-cadherin promoter suppression in SW480-ZEB2 cells.

Zheng Y, et al. Cancers (Basel). 2022 Jul 14;14(14):3426.

Pemrametostat (GSK3326595) Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Biological Activity

Description Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
Targets
PRMT5 [1]
In vitro
In vitro

Both GSK3326595 and Santacruzamate A treatments rescue the ZEB2-mediated E-cadherin promoter suppression in SW480-ZEB2 cells, confirming that the ZEB2-mediated repression of E-cadherin in CRC cells is facilitated by PRMT5 and HDAC2.[2]
Cell Research Cell lines SW480 cells
Concentrations 100, 250, 500 nM
Incubation Time 48 h
Method

SW480+Vector and SW480+ZEB2 cells express plasmid pGL3-E-cadherin promoter-Luc. InPRMT5 (GSK3326595) and inHDAC2 (Santacruzamate A) were added to the cell medium, and luciferase activity was assayed, 48 h later, luciferase activity was assayed and normalized to Renilla. (E) SW620 cells express plasmid pGL3-E-cadherin promoter-Luc. InPRMT5 (GSK3326595) and inHDAC2 (Santacruzamate A) were added to the medium, and luciferase activity was assayed, 48 h later, luciferase activity was assayed and normalized to Renilla.

(Data sourced from selleck products)
Experimental Result Images Methods Biomarkers Images PMID
Western blot H4R3me2s MDM4 31439820
In Vivo
In vivo

GSK3326595 reduces liver metastasis of CRC cells and completely inhibits the distant metastasis of SW620 cells in nude mice.[2]
Animal Research Animal Models Female BALB/c nude mice injected with SW620
Dosages 100 mg/kg
Administration i.v.

(Data sourced from selleck products)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04676516 Completed
Breast Cancer
Ottawa Hospital Research Institute|Ontario Institute for Cancer Research|GlaxoSmithKline|London Regional Cancer Program Canada|Hamilton Health Sciences Corporation
 June 8 2021 Phase 2
NCT03614728 Terminated
Neoplasms
GlaxoSmithKline
 October 16 2018 Phase 1|Phase 2
NCT02783300 Completed
Neoplasms
GlaxoSmithKline
 August 30 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 452.55 Formula

C24H32N6O3
CAS No. 1616392-22-3 SDF Download Pemrametostat (GSK3326595) SDF
Smiles CC(=O)N1CCC(CC1)NC2=NC=NC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (201.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 32 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

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.
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.

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.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595) supplier | purchase Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595) cost | Pemrametostat (GSK3326595) manufacturer | order Pemrametostat (GSK3326595) | Pemrametostat (GSK3326595) distributor