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Formula | C24H32N6O3 |
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Molecular Weight | 452.55 | CAS No. | 1616392-22-3 | |
Solubility (25°C)* | In vitro | DMSO | 91 mg/mL (201.08 mM) | |
Ethanol | 32 mg/mL (70.71 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.) |
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. | |
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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] |
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In vivo | GSK3326595 reduces liver metastasis of CRC cells and completely inhibits the distant metastasis of SW620 cells in nude mice.[2] |
Cell Assay: |
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Animal Study: |
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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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.