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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
| Related PRMTs Products |
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| C7280948
C7280948 is an inhibitor of histone arginine methyltransferase PRMT1 with IC50 values of 12.75 uM. |
| EPZ015666
EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
| SGC707
SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. |
| EPZ020411
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8. |
| XY1
XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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