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LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.
| Molecular Weight | 342.35 |
| Formula | C17H18N4O4 |
| CAS Number | 2040291-27-6 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] H. Ümit Kaniskan, et al. Chem Rev. Inhibitors of Protein Methyltransferases and Demethylases
| 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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