SKLB-03176

SKU: orb2279951

Description

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells.

Key Properties

• CAS Number: 2609675-22-9
• MW: 514.618666172028
• Purity: >98%
• Formula: C₂₉H₃₄N₆O₃
• SMILES: C(C1=C(C(NC(=O)C=C)=CC(C2=CN=C(N3CCNCC3)C=C2)=C1)C)(=O)NCC1C(NC(C)=CC=1CC)=O

Storage & Handling

• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

168285936