GSK343

The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases. GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM. See Structural Genomics Consortium (SGC) website for more information.Formal Name: N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide. CAS Number: 1346704-33-3. Molecular Formula: C31H39N7O2. Formula Weight: 541.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 1 mg/ml, Ethanol: 2 mg/ml. lambdamax: 256, 305 nm. SMILES: CC(C)N(N=C1)C2=C1C(C(NCC3=C(CCC)C=C(C)NC3=O)=O)=CC(C4=CC(N5CCN(C)CC5)=NC=C4)=C2. InChi Code: 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). InChi Key: ULNXAWLQFZMIHX-UHFFFAOYSA-N.