Compound name
A-395
Protein family
Methyltransferase
Target name
EED
Affinity biochemical (nM)
0.4
Affinity on-target cellular (nM)
90
CG-Set
Other targets set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000219b
SMILES
CN(C)[C@H]1CN(C2CCc3cccc(F)c32)C[C@@H]1c1ccc(N2CCN(S(C)(=O)=O)CC2)cc1
InChIKey
REVJNSVNICWODC-KIDMSAQOSA-N
NCBI gene ID
8726
UniProt ID
O75530
Synonyms
WAIT-1, HEED
Mode of action
Inhibitor
Negative control
A-395N
Affinity biochemical definition
Ki
Affinity biochemical assay type
TR-FRET binding assay
Affinity Biochemical Source Knowledge
https://www.nature.com/articles/nchembio.2306
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
AlphaLISA assay (inhibition of H3K27me3 formation in RD Rhabdoid tumor cell line)
Affinity on-target cellular source knowledge
https://www.nature.com/articles/nchembio.2306
Affinity on-target cellular relation
=
Selectivity platform
Scintillation proximity assay (SPA)
Selectivity platform number of targets
32
Selectivity remarks
Screened at 1 µM and 50 µM against epigenetic methyltransferases including lysine, arginine, and DNA methyltransferases: clean selectivity profile with all targets >80% remaining activity, https://www.thesgc.org/chemical-probes/A-395; Screened in DSF assays, at 0.5 mM and 1 mM, against 8 epigenetic ‘reader domain' proteins: dTm(53BP1) <2 K, dTm(BRPF3) <2 K, dTm(DNMT3A) <2 K, dT,(RBBP1) <2 K, dTm(RBPF1) <2 K, dTm(UHRF1) <2 K, dTm(WDR5) <2 K, dTm(WHSC1L1) <2 K, https://pubmed.ncbi.nlm.nih.gov/28135237/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28135237/
Selectivity Number of Off-targets
0