//php if ($breadcrumb): print $breadcrumb; endif; ?>

Chemical Probes Portal GSK343.pdf
GSK343

Reagent Authentication Certificate:

Protein target name:
EZH2Mechanism of action:
competitive with SAMRecommended Concentration for use in cells:
100 nM - 3 uM
Probe Availability
Probe Information
In vitro validation
Potency:
Ki (app)1.2 nM
Potency assay:
for SAM bindingOff target protein and potency:
EZH1 IC50 = 0.24 uMPotency assay (off target):
EZH2 IC50 = 0.004 uM; SET7 IC50 = 63 uM; PRMT3 IC50 = 74 uM;
All others IC50 > 100 uM (DNMT1, DNMT3A, DNMT3B, DOT1L, KMT2A, KMT2D, KMT2C, KMT2B, PRMT1, PRMT4, PRMT5, SETMAR, KMT5B, KMT5C, EHMT2)In cell validation
Potency in cells:
IC50174 nM
Potency assay (cells):
in-cell protein substrate methylation assayTarget engagement assay (cells):
Indirect, in-cell protein substrate methylation assayExternal Resources
Available data:
GDSC2