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AMI-1 is a potent and selective, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50 values of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 is also a potent scavenger of NADPH-oxidase-derived superoxide. AMI-1 specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site. AMI-1 inhibits methylation of GFP-Npl3 and cellular proteins.
In vivo, AMI-1 (5 μg/rat) in chronic AIPI rats ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs.
| Molecular Weight | 548.45 |
| Formula | C21H14N2Na2O9S2 |
| CAS Number | 20324-87-2 |
| Solubility (25°C) | DMSO 45 mg/mL Water 10 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 |
|---|
| 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. |
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