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GSK591 (EPZ015866) is a SGC probe for PRMT5. GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5/MEP50 complex. GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 of 56 nM.
Acta Pharm Sin B. 2024 Nov 05.
Tumor-intrinsic PRMT5 upregulates FGL1 via methylating TCF12 to inhibit CD8+ T-cell-mediated antitumor immunity in liver cancer
GSK591 purchased from AbMole
| Molecular Weight | 380.48 |
| Formula | C22H28N4O2 |
| CAS Number | 1616391-87-7 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Jianhao Huang, et al. PRMT5 Promotes EMT Through Regulating Akt Activity in Human Lung Cancer
[3] Patty Sachamitr, et al. PRMT5 inhibition disrupts splicing and stemness in glioblastoma
[5] Shikui Zhang, et al. Targeting PRMT5/Akt signalling axis prevents human lung cancer cell growth
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Products are for research use only. Not for human use. We do not sell to patients.
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