Compound name
PFI-2
Protein family
HMT
Target name
SETD7
Affinity biochemical (nM)
2
Affinity on-target cellular (nM)
10000
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000196bCl
SMILES
Cl.O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1
InChIKey
ZADKZNVAJGEFLC-ZMBIFBSDSA-N
NCBI gene ID
80854
UniProt ID
Q8WTS6
Synonyms
KMT7, SET7, SET7/9, SET9
Mode of action
Inhibitor
Negative control
(S)-PFI-2
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation proximity assay (SPA)
Affinity Biochemical Source Knowledge
https://doi.org/10.1073/pnas.1407358111
https://www.thesgc.org/chemical-probes/PFI-2
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Immunoblot (increase in nuclear YAP levels by treatment of MEFs (from Setd7+/+ mice) with 10 µM PFI-2)
Affinity on-target cellular relation
<
Selectivity platform
Methyltransferase panel, literature
Selectivity platform number of targets
19
Selectivity remarks
Screened at 50 µM, >1000-fold selective over other methyltransferases (G9a, EZH2, EHMT1, SUV39H2, EZH1, SUV420H1, SUV420H2, SETD8, SETD2, PRMT1, PRMT3, PRMT5, PRMT8, SETDB1, MLL1, DOT1L, WHSC1, SMYD2, DNMT1); Screened against 137 ion channels, GPCRs, and enzymes at 10 µM, closest targets: Ki(A2B) = 1.3 µM, Ki(BB3) = 8.1 µM, Ki(motilin) = 7.2 µM, Ki(KOP) = 3.8 µM
Selectivity Source Knowledge
https://doi.org/10.1073/pnas.1407358111
Selectivity Number of Off-targets
0