Compound name
PFI-6
Protein family
YEATS
Target name
MLLT3
Affinity biochemical (nM)
160
Affinity on-target cellular (nM)
760
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000731a
SMILES
O=C(N(C)C)C1=C(O)C=C(C2=CC(C(N[C@@H]3CCC4=C3C=CC=C4)=O)=NO2)C=C1
InChIKey
IXWUILRSNIQHDM-QGZVFWFLSA-N
NCBI gene ID
4300
UniProt ID
P42568
Synonyms
AF-9 AF9 YEATS3
Mode of action
Inhibitor
Negative control
PFI-6N
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF-based inhibition assay
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/PFI-6
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity remarks
Selective in SGC bromodomain panel; Screened in Invitrogen kinase panel against 40 kinases at 10 µM, clean profile; No activity in a panel of 25 PDEs, ion channels and GPCRS, IC50 >50 µM; IC50(YEATS2/4) > 40 µM (HTRF assay);
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/PFI-6