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CID 5380390 is a selective inhibitor of Protein Arginine Methyltransferases PRMT1 and PRMT8. PRMT1 is responsible for the majority of arginine methylation in the cell involved in transcription, chromatin modification, and signal transduction. CID 5380390 has an IC50 values of 23 μM for PRMT1, and does not inhibit PRMTs 3, 4, and 6, although it does inhibit PRMT8. The mechanism is believed to involve a specific S-adenosylmethionine (SAM)-binding cysteine present only in the Type I PRMTs PRMT1 and PRMT8 and absent in other SAM-dependent methyltransferases.
| Molecular Weight | 209.2 |
| Formula | C10H11NO4 |
| CAS Number | 37630-20-9 |
| Solubility (25°C) | DMSO 15 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. |
| 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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