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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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| AMG-193
AMG-193 is an orally active inhibitor of the PRMT5/MTA complex for studies related to solid tumors. AMG-193 (PRMT5-IN-27) inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM. |
| AZD3470
AZD3470 is a novel PRMT5 inhibitor targeting the MTA and PRMT5 complex for studies related to hematologic tumors. |
| TNG-462
TNG-462 is an orally active PRMT5 inhibitor for investigation of MTAP-deficient and/or MTA-accumulating cancers. |
| TNG908
TNG908 (Ralometostat) is a PRMT5 inhibitor that crosses the blood-brain barrier and can be used in studies related to advanced solid tumors. |
| PRMT5-IN-20
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity. |
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