1848944-46-6
Chemical Structure
Pemrametostat succinate
Synonym(s): GSK3326595 succinate; EPZ015938 succinate
- CAS No.: 1848944-46-6
- Formula:C28H38N6O7
- Molecular Weight:570.64
InChIKey: GXLSVNOMQNNGQM-BOXHHOBZSA-N
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
Biological Activity: 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[1][2][3][4][5].
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Pemrametostat succinate | 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. | |||||||||||||||||||||
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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]
