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SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM. SGC707 binds to PRMT3 and reduces PRMT3-dependent H4R3me2a. SGC707 also stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively. SGC707 (30 mg/kg, i.p.) gives good plasma exposure over 6 h with the peak plasma level of 38000 nM in CD-1 male mice, which suggests that SGC707 is suitable for animal studies.
| Molecular Weight | 298.34 |
| Formula | C16H18N4O2 |
| CAS Number | 1687736-54-4 |
| Solubility (25°C) | DMSO 49 mg/mL Ethanol 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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. |
| 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. |
| SGC2085
SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. |
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