Description
A potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC₅₀ = 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC₅₀ of <200nM (measured by immunofluorescence).
GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC₅₀ = 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity).
Alternate Name/Synonyms: 1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridine-4-yl)-1H-indazole-4-carboxamide
Appearance: Crystalline solid
Formulation: N/A
CAS Number: N/A
Structure Available?: Yes
Peptide sequence: No
Salt Form: No
Molecular Formula: C₃₁H₃₉N₇O₂
Molecular Weight: 541.69
Cell-Permeable?: Yes
Purity: ≥99% by HPLC
Solubilities: DMSO
Handling: Protect from light and moisture
Country of Origin: USA
Tag Line: A potent EZH2 inhibitor
MDL Number: N/A
PubChem CID: 71268957
SMILES: CCCC1=C(CNC(=O)C2=C3C=NN(C(C)C)C3=CC(=C2)C2=CC=NC(=C2)N2CCN(C)CC2)C(=O)NC(C)=C1
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)
InChi Key: ULNXAWLQFZMIHX-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20 ̊C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |