Pemrametostat (GSK3326595)

Catalog No.S8664 Batch:S866404

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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 20 mg/mL (44.19 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.55mg/ml Taking the 1 mL working solution as an example, add 50 μL of 91 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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)

Selleck's Pemrametostat (GSK3326595) has been cited by 19 publications

A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52] PubMed: 38413740
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
Ribosome subunit attrition and activation of the p53-MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition [ bioRxiv, 2023, 2023.07.26.550648] PubMed: 37546802
Ribosome subunit attrition and activation of the p53-MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition [ bioRxiv, 2023, 2023.07.26.550648] PubMed: 37546802

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.