For research use only. Not for therapeutic Use.
LLY-283 (CAT: I014449) is a potent and selective chemical probe that competitively targets the S-adenosylmethionine (SAM) binding site of PRMT5 (protein arginine methyltransferase 5). As an oral PRMT5 inhibitor, LLY-283 exhibits significant potency, with an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex. It demonstrates strong antitumor activity, suggesting its potential as a therapeutic agent in cancer treatment. By selectively inhibiting PRMT5, LLY-283 may interfere with the methylation of arginine residues, which can impact cellular processes involved in tumor growth and progression.
| Catalog Number | I014449 |
| CAS Number | 2040291-27-6 |
| Synonyms | LLY-283; LLY 283; LLY283; LM-5179; LM 5179; LM5179.;(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol |
| Molecular Formula | C17H18N4O4 |
| Purity | ≥95% |
| Target | Histone Methyltransferase |
| Solubility | Soluble in DMSO |
| IUPAC Name | (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol |
| InChI | InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12+,13-,14-,17-/m1/s1 |
| InChIKey | WWOOWAHTEXIWBO-QFRSUPTLSA-N |
| SMILES | O[C@H]1[C@H](N2C=CC3=C(N)N=CN=C32)O[C@H]([C@H](O)C4=CC=CC=C4)[C@H]1O |
| Reference | <span style=”color:#000000;”><span style=”font-family:arial,helvetica,sans-serif;”><span style=”font-size:12px;”>1.Bonday, Zahid Q., et al. "LLY-283, a potent and selective inhibitor of arginine methyltransferase 5, PRMT5, with antitumor activity." <i style=”font-family: Arial, sans-serif; font-size: 13px;”>ACS medicinal chemistry letters</i> 9.7 (2018): 612-617.</span></span></span> |
