For research use only. Not for therapeutic Use.
GSK321 (Cat No.: I007103) is a small-molecule inhibitor developed by GlaxoSmithKline, designed to selectively target and inhibit the function of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase involved in gene silencing via trimethylation of H3K27. EZH2 is often overexpressed in various cancers, contributing to tumor progression and therapy resistance. By blocking EZH2 activity, GSK321 reactivates silenced tumor suppressor genes and inhibits cancer cell proliferation. It is widely used in epigenetic and oncology research to explore targeted cancer treatment strategies.
| CAS Number | 1816331-63-1 |
| Synonyms | (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide |
| Molecular Formula | C28H28FN5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H28FN5O3/c1-17-14-33(28(37)24-7-4-12-30-24)16-23-25(27(36)31-22-6-3-5-20(13-22)18(2)35)32-34(26(17)23)15-19-8-10-21(29)11-9-19/h3-13,17-18,30,35H,14-16H2,1-2H3,(H,31,36)/t17-,18+/m1/s1 |
| InChIKey | IVFDDVKCCBDPQZ-MSOLQXFVSA-N |
| SMILES | CC1CN(CC2=C1N(N=C2C(=O)NC3=CC=CC(=C3)C(C)O)CC4=CC=C(C=C4)F)C(=O)C5=CC=CN5 |
| Reference | [1]. Ujunwa C Okoye-Okafor, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86. [2]. Stuart Jones, et al. Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells. J Med Chem. 2016 Dec 22;59(24):11120-11137. |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
