For research use only. Not for therapeutic Use.
GSK343（Cat No.:I001337）is a selective inhibitor of the histone methyltransferase EZH2, a critical component of the Polycomb repressive complex 2 (PRC2) that regulates gene expression through trimethylation of histone H3 at lysine 27 (H3K27me3). By inhibiting EZH2, GSK343 reactivates silenced tumor suppressor genes and disrupts pathways associated with cancer cell proliferation and survival. This compound has shown promising anti-cancer effects in preclinical studies, particularly in hematologic malignancies and solid tumors characterized by high EZH2 expression. GSK343’s ability to modulate epigenetic changes makes it a significant candidate for targeted cancer therapies.
| Catalog Number | I001337 |
| CAS Number | 1346704-33-3 |
| Synonyms | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide |
| Molecular Formula | C31H39N7O2 |
| Purity | ≥95% |
| Target | EZH2 |
| Solubility | DMSO: ≥ 31 mg/mL |
| Storage | Store at -20°C |
| IC50 | 4 nM |
| IUPAC Name | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide |
| InChI | InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40) |
| InChIKey | ULNXAWLQFZMIHX-UHFFFAOYSA-N |
| SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C |
| Reference | </br>1:Fuse-binding protein 1 is a target of the EZH2 inhibitor GSK343, in osteosarcoma cells. Xiong X, Zhang J, Liang W, Cao W, Qin S, Dai L, Ye D, Liu Z.Int J Oncol. 2016 Aug;49(2):623-8. doi: 10.3892/ijo.2016.3541. Epub 2016 May 27. PMID: 27278257 </br>2:In silico and experimental analyses predict the therapeutic value of an EZH2 inhibitor GSK343 against hepatocellular carcinoma through the induction of metallothionein genes. Liu TP, Hong YH, Tung KY, Yang PM.Oncoscience. 2016 Jan 29;3(1):9-20. eCollection 2016. PMID: 26973856 Free PMC Article |
