DC Chemicals · Product datasheet

SKLB-03176 — Datasheet

CAT. NO. DC70785

Product page and current package options

ParameterValue
Chemical NameSKLB-03176
CAS No.2609675-22-9
SynonymsSKLB-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
FormulaC29H34N6O3
M.Wt514.618666172028
SMILESC(C1=C(C(NC(=O)C=C)=CC(C2=CN=C(N3CCNCC3)C=C2)=C1)C)(=O)NCC1C(NC(C)=CC=1CC)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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.

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Cart

Request quotation