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: 1616392-22-3

Selleck's Pemrametostat (GSK3326595) has been cited by 16 publications

Purity & Quality Control

Batch: Purity: 99.85%
99.85

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.

Fulvestrant


Pemrametostat and Fulvestrant synergistically inhibit growth of ER+/RB-deficient patient-derived xenografts.

Lin CC, et al. Res Sq. 2023 Jul 10;rs.3.rs-2966905.

Palbociclib


Pemrametostat enhances the efficacy of Palbociclib and results in more profound growth inhibition in the A375 and HT144 cell lines.

AbuHammad S, et al. Proc Natl Acad Sci U S A. 2019 Sep 3;116(36):17990-18000.

Niraparib (MK-4827)


Pemrametostat and Niraparib use results in increased anti-tumor activity in vitro and in vivo.

O'Brien S, et al. BMC Cancer. 2023 Aug 18;23(1):775.

Abemaciclib


Pemrametostat and Abemaciclib treatment exhibits more profound tumor suppression in Maver-1-derived CDX model.

Che Y, et al. Blood Cancer J. 2023 Feb 17;13(1):27.

Pemrametostat (GSK3326595) Related Products

Choose Selective Histone Methyltransferase Inhibitors

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


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In vivo
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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.

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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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