GSK343

• CAT Number: I001337
• CAS Number: 1346704-33-3
• Molecular Formula: C31H39N7O2
• Molecular Weight: 541.7
• Purity: ≥95%
• Target: EZH2
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: Store at -20°C
• IC50: 4 nM [1]
• 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

GSK343 (Cat.No:I001337) is a selective inhibitor of the histone lysine methyltransferase enzyme, EZH2. It has been extensively studied for its potential in epigenetic modulation and cancer therapy. GSK343 specifically targets and inhibits EZH2, leading to the suppression of abnormal gene expression patterns and potential anti-tumor effects. Clinical investigations are ongoing to explore its therapeutic applications.

Reference

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 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