Pemrametostat (GSK3326595)

Catalog No.S8664 Batch:S866403

Technical Data

Formula	C₂₄H₃₂N₆O₃
Molecular Weight	452.55	CAS No.	1616392-22-3
Solubility (25°C)*	In vitro	DMSO	91 mg/mL (201.08 mM)
		Ethanol	91 mg/mL (201.08 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

In vivo

GSK3326595 reduces liver metastasis of CRC cells and completely inhibits the distant metastasis of SW620 cells in nude mice.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	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)
Animal Study:^{^[2]}	Animal Models Female BALB/c nude mice injected with SW620 Dosages 100 mg/kg Administration i.v. (Data sourced from selleck products)

Cell Assay:^{^[2]}

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)

Animal Study:^{^[2]}

Animal Models
Female BALB/c nude mice injected with SW620
Dosages
100 mg/kg
Administration
i.v.

(Data sourced from selleck products)

References

Selleck's Pemrametostat (GSK3326595) has been cited by 21 publications

A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52]	PubMed: 38413740
Ribosome subunit attrition and activation of the p53-MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition [ Elife, 2024, 12RP90683]	PubMed: 38682900
Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers [ J Med Chem, 2024, 67(8):6064-6080.]	PubMed: 38595098
Metabolic rewiring induced by ranolazine improves melanoma responses to targeted therapy and immunotherapy [ Nat Metab, 2023, 10.1038/s42255-023-00861-4]	PubMed: 37563469
Metabolic rewiring induced by ranolazine improves melanoma responses to targeted therapy and immunotherapy [ Nat Metab, 2023, 5(9):1544-1562]	PubMed: 37563469
MST2 methylation by PRMT5 inhibits Hippo signaling and promotes pancreatic cancer progression [ EMBO J, 2023, e114558.]	PubMed: 37905571
PRMT5 reduces immunotherapy efficacy in triple-negative breast cancer by methylating KEAP1 and inhibiting ferroptosis [ J Immunother Cancer, 2023, 11(6)e006890]	PubMed: 37380368
PRMT5 triggers glucocorticoid-induced cell migration in triple-negative breast cancer [ Life Sci Alliance, 2023, 6(10)e202302009]	PubMed: 37536978
PRMT5/FGFR3/AKT Signaling Axis Facilitates Lung Cancer Cell Metastasis [ Technology in Cancer Research & Treatment, 2023, 10.1177/15330338231161139]	PubMed: None
PRMT5/FGFR3/AKT Signaling Axis Facilitates Lung Cancer Cell Metastasis [ Technol Cancer Res Treat, 2023, 22:15330338231161139]	PubMed: 36927233

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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