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SKLB-03176

  Cat. No.:  DC70785   Featured
Chemical Structure
2609675-22-9
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2609675-22-9
Chemical Name: SKLB-03176
Synonyms: SKLB-03176;N-[(4-Ethyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-3-[(1-oxo-2-propen-1-yl)amino]-5-[6-(1-piperazinyl)-3-pyridinyl]benzamide
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
Formula: C29H34N6O3
M.Wt: 514.618666172028
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
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DC70785 SKLB-03176 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.
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DC47616 EPZ-719 EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.
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DC46276 BRD0639 BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.
DC44514 MR837(ZINC30303842) MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain).
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