Cat. No.: HY-101563A

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Pemrametostat succinate

Name: Pemrametostat succinate
Brand: MedChemExpress
SKU: HY-101563A
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(Synonyms: GSK3326595 succinate; EPZ015938 succinate)

33 Cited Publications

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Based on 33 publication(s) in Google Scholar

GSK3326595 succinate (EPZ015938 succinate) is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 succinate decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 succinate can be used for research of relapsed/refractory mantle cell lymphoma.

For research use only. We do not sell to patients.

CAS No.: 1848944-46-6
Formula: C₂₈H₃₈N₆O₇
Molecular Weight:570.64

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Pemrametostat succinate Chemical Structure

CAS No.: 1848944-46-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (33)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PRMT5

CDK4

CDK6

All Histone Methyltransferase Isoforms :

All CDK Isoforms :

In Vitro

GSK3326595 (10-100 nM, 24-72 h) succinate (EPZ015938 succinate) inhibits SARS-CoV-2spike pseudovirus infection HEK-293 cells and A549 cells by attenuating ACE2-RBD interaction^[1].
GSK3326595 (100 nM, 12 h) succinate primes peritoneal macrophages to IFN-gamma-induced M1 polarization^[3].
GSK3326595 (0.15-10 μM, 72 h) succinate induces cell death in MCL cell^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[4]

Cell Line:

HEK-293T cells, A549 cells
Concentration:

10 nM, 25 nM, 50 nM, 100 nM
Incubation Time:

48 h
Result:

Strongly inhibited ACE2-RBD interaction at low concentration.
Inhibited SARS-CoV-2 Omicron and other variants Spike1 binding with ACE2.
Inhibits SARS-CoV-2 spike pseudovirus infection host cells.

Cell Cytotoxicity Assay^[1]

Cell Line:

MCL cells
Concentration:

0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:

72 h
Result:

Resulted in modest growth inhibition in MCL cells.

In Vivo

GSK3326595 (5 mg/kg, Intraperitoneal injection, three times a week for 9 weeks) succinate (EPZ015938 succinate) increased hepatic triglyceride levels without affecting atherosclerosis in LDL receptor knockout mice^[3].
GSK3326595 (25-50 mg/kg, Oral, once a day for 2 weeks) succinate enhances the efficacy of anti-programed cell death protein 1 (PD-1) immune checkpoint therapy (ICT) in hepatocellular carcinoma (HCC) in myelocytomatosis transgene turned on (MYC-ON) mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

LDL receptor knockout mice^[3]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Did not alter atherosclerosis susceptibility.
Increased hepatic triglyceride levels without changing the hyperlipidemia extent.
Activated genes involved in fatty acid acquisition.

Animal Model:

myelocytomatosis transgene turned on mice^[5]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

Oral
Result:

Significantly suppressed tumor growth at 50 mg/kg.
Showed better therapeutic efficacy at 25 mg/kg.

Chemical Information

CAS No. 1848944-46-6
Molecular Weight 570.64
Formula C₂₈H₃₈N₆O₇
SMILES

OC(CCC(O)=O)=O.O=C(C1=NC=NC(NC2CCN(CC2)C(C)=O)=C1)NC[C@H](O)CN3CC4=CC=CC=C4CC3
Synonyms

GSK3326595 succinate; EPZ015938 succinate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (33)

All Cell Proliferation/Viability AssayWBIHC

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Gut

Identification of PRMT5 as a therapeutic target in cholangiocarcinoma. [Abstract]

2024 Sep 11:gutjnl-2024-332998. PMID: 39266051

Pemrametostat succinate purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

GI₅₀ values for the PRMT5 inhibitors GSK3326595 and JNJ64619178 (Onametostat) in the indicated CCA cell lines.

Pemrametostat succinate purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

Immunoblot analysis of PRMT5-dependent symmetric dimethylarginine (SMDA) protein marks in control and GSK3326595 or JNJ64619178 (Onametostat) treated HuCCT-1 and TFK-1 cells at the indicated doses for 5 days.

Pemrametostat succinate purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

Immunohistochemical analysis of CK19 and H&E stainings showing the extent of CCA lesions in control Jnk^Δhepa+DEN+CCl4 and GSK3326595-treated mice. Representative images are shown.
Nat Commun

A BRET biosensor for measuring uncompetitive engagement of PRMT5 complexes in cells. [Abstract]

2025 Dec 3;16(1):10129. PMID: 41339334
Nat Commun

PRMT5-mediated arginine methylation activates AKT kinase to govern tumorigenesis. [Abstract]

2021 Jun 8;12(1):3444. PMID: 34103528

Pemrametostat succinate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 8;12(1):3444. [Abstract]

Breast cancer cells are treated with DMSO, 0.5 μM GSK3326595 (GSK) for 4 days before examining cell viability.
J Adv Res

The aryl hydrocarbon receptor inhibits antigen presentation to promote progression of pancreatic ductal adenocarcinoma. [Abstract]

2025 Nov 5:S2090-1232(25)00874-4. PMID: 41203070
J Exp Clin Cancer Res

Flavokawain A is a natural inhibitor of PRMT5 in bladder cancer. [Abstract]

2022 Oct 5;41(1):293. PMID: 36199122
Adv Sci (Weinh)

Zinc Alleviates Gut Barrier Dysfunction by Promoting the Methylation of AKT. [Abstract]

2025 Sep;12(33):e08280. PMID: 40642900

Pemrametostat succinate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep;12(33):e08280. [Abstract]

HCT116 cells were treated with GSK3326595 (10 μM) for 6 h,HCT116 cells were starved in amino acid-free medium for 1 h, and then supplemented with ZnSO₄ for the indicated time. The level of pS473-AKT,binding
MedComm (2020)

SCR-7952, a highly selective MAT2A inhibitor, demonstrates synergistic antitumor activities in combination with the S-adenosylmethionine-competitive or the methylthioadenosine-cooperative protein arginine methyltransferase 5 inhibitors in methylthioadenosine phosphorylase-deleted tumors. [Abstract]

2024 Sep 20;5(10):e705. PMID: 39309689
Cell Death Dis

Reversible arginine methylation regulates mitochondrial IDH2 activity: coordinated control by CARM1 and KDM3A/4A. [Abstract]

2026 Feb 2;17(1):195. PMID: 41629283
Cancer Lett

DysUFMylation reprograms immunosuppressive neutrophils to potentiate anti-PD-1 therapy in hepatocellular carcinoma. [Abstract]

2026 May 1:645:218395. PMID: 41780840
Clin Cancer Res

MTA-Cooperative PRMT5 Inhibitors are Efficacious in MTAP-Deleted Malignant Peripheral Nerve Sheath Tumor Models. [Abstract]

2025 Jun 24. PMID: 40553452
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
EMBO Mol Med

Nuclear PRMT5 is a biomarker of sensitivity to tamoxifen in ERα+ breast cancer. [Abstract]

2023 Aug 7;15(8):e17248. PMID: 37458145
Blood Adv

Loss of METTL3 attenuates blastic plasmacytoid dendritic cell neoplasm response to PRMT5 inhibition via IFN signaling. [Abstract]

2022 Apr 28;bloodadvances.2021006306. PMID: 35482445
Cell Mol Life Sci

Opposing USP19 splice variants in TGF-β signaling and TGF-β-induced epithelial-mesenchymal transition of breast cancer cells. [Abstract]

2023 Jan 17;80(2):43. PMID: 36646950
Biomed J

PRMT5-mediated methylation of LKB1 controls PD-L1 expression in NSCLC. [Abstract]

2026 Jun 10:101002. PMID: 42270077
EMBO Rep

Arginine methylation-dependent METTL14-SMN interaction regulates RNA m6A homeostasis. [Abstract]

2025 Oct 6. PMID: 41053315
Invest Ophthalmol Vis Sci

PRMT5 Regulates Senescence in Retinal Ganglion Cells by Targeting the Wnt/β-Catenin Signaling Cascade. [Abstract]

2025 Jun 2;66(6):8. PMID: 40459496
Transl Oncol

TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]

2025 Feb:52:102264. PMID: 39756156
Sci Rep

Autophagy dictates sensitivity to PRMT5 inhibitor in breast cancer. [Abstract]

2023 Jul 3;13(1):10752. PMID: 37400460
Cancers (Basel)

TRAF6 Promotes PRMT5 Activity in a Ubiquitination-Dependent Manner. [Abstract]

2023 Apr 27;15(9):2501. PMID: 37173967
J Cell Mol Med

PRMT5 activates KLF5 by methylation to facilitate lung cancer. [Abstract]

2024 Mar;28(5):e17856. PMID: 37461162
J Biol Chem

Protein arginine methyltransferase 5 is essential for oncogene product EWSR1-ATF1-mediated gene transcription in clear cell sarcoma. [Abstract]

2022 Oct;298(10):102434. PMID: 36041632
Breast Cancer (Dove Med Press)

Therapeutic Advantage of Targeting PRMT5 in Combination with Chemotherapies or EGFR/HER2 Inhibitors in Triple-Negative Breast Cancers. [Abstract]

2023 Nov 6:15:785-799. PMID: 37954171
Mol Carcinog

PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]

2023 Aug;62(8):1119-1135. PMID: 37144835
Glycobiology

Compromised CDK12 activity causes dependency on the high activity of O-GlcNAc transferase. [Abstract]

2024 Dec 10;34(12):cwae081. PMID: 39361894
bioRxiv

2026 Apr 13.
bioRxiv

Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]

2026 Feb 18:2026.02.16.706212. PMID: 41757027
SSRN

2025 Dec 1.
Res Sq

2025 Jul 14.
bioRxiv

Ribosomal RNA transcription governs splicing through ribosomal protein RPL22. [Abstract]

2024 Aug 16:2024.08.15.608201. PMID: 39211199
Medical University of South Carolina

2023 Aug 12.
Research Square Print

November 11th, 2022.
Springer

2021 May 12.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Che Y, et al. Exploiting PRMT5 as a target for combination therapy in mantle cell lymphoma characterized by frequent ATM and TP53 mutations [J]. Blood cancer journal, 2023, 13(1): 27. [Content Brief]

[2]. Fedoriw A, et al. Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP loss [J]. Cancer cell, 2019, 36(1): 100-114. e25.

[3]. Zhang Y, et al. PRMT5 inhibition induces pro‐inflammatory macrophage polarization and increased hepatic triglyceride levels without affecting atherosclerosis in mice [J]. Journal of Cellular and Molecular Medicine, 2023, 27(8): 1056-1068.

[4]. Li Z, et al. GSK3326595 is a promising drug to prevent SARS-CoV-2 Omicron and other variants infection by inhibiting ACE2-R671 di-methylation [J]. Journal of Medical Virology, 2023, 95(1): e28158.

[5]. Luo Y, et al. Myelocytomatosis-protein arginine N-methyltransferase 5 Axis defines the tumorigenesis and immune response in hepatocellular carcinoma [J]. Hepatology, 2021, 74(4): 1932-1951. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Pemrametostat succinate

33 Cited Publications

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Pemrametostat succinate

Publications Citing Use of MedChemExpress (MCE) Pemrametostat succinate

All Histone Methyltransferase Isoforms

All CDK Isoforms