Epigenetics Probes Collection

The study of post-translational modification (PTM) of lysine and/or arginine residues in histones and other proteins through methylation and acetylation has led to the discovery of three classes of epigenetic proteins:-

  1. Those which add a methyl or acetyl group (writers) using S-adenosylmethionine (methylation) and Acetyl-CoA (acetylation) as co-factors. Histone methyltransferases catalyze the transfer of up to three methyl groups to the e-amino group of a lysine residue or up to two methyl groups to the guanidine group of an arginine residue. In the case of arginine methylation, dimethylation can occur in a symmetrical or unsymmetrical manner.  Acetylation of lysine residues only occurs once and arginines are not acetylated.
  2. Those which remove a methyl or acetyl group (erasers).
  3. Those which bind histones/proteins containing a particular PTM (readers).

Each of these classes of epigenetic proteins contributes to the control of various genes and the goal of the Epigenetic Probes Project is to unravel the biology of these proteins by developing small-molecule inhibitors and antagonists with the following properties

  • IC50 or Kd < 100nM
  • Selectivity > 30-fold over proteins in the same family
  • Significant cellular activity below 1 microM

 Brochure - SGC Epigenetic Chemical Probes ( September 2015 )


Name Structure Protein Family Specific Targets Control In vivo parameters tested* Addedsort ascending
GSK864 Dehydrogenase Mutant isocitrate dehydrogenase 1 GSK990 yes 11/15
A-196 Histone Methyltransferase SUV420H1/H2 A-197 no 07/15
GSK591 Histone Methyltransferase PRMT5 no 07/15
MS023 Histone Methyltransferase Type I PRMTs MS094 no 07/15
MS049 Histone Methyltransferase PRMT4,6 no 06/15
NVS-CECR2-1 Bromodomains CECR2 no 06/15
I-BRD9 Bromodomains BRD9 no 05/15
BI-9564 Bromodomains BRD9, BRD7 yes 04/15
BAY-598 Histone Methyltransferase SMYD2 yes 04/15
GSK484 Arginine deiminases PAD-4 GSK106 yes 03/15
GSK2801 Bromodomains BAZ2A, BAZ2B GSK8573 yes 12/14
LP99 Bromodomains BRD9, BRD7 2S,3R-enantiomer no 12/14
NI-57 Bromodomains BRPF1, BRPF2, BRPF3 no 12/14
PFI-4 Bromodomains BRPF1B no 12/14
OF-1 Bromodomains BRPF1, BRPF2, BRPF3 no 07/14
SGC707 Histone Methyltransferase PRMT3 XY1 no 06/14
BAZ2-ICR Bromodomains BAZ2A, BAZ2B yes 05/14
OICR-9429 WD40 WDR5 OICR-0547 no 05/14
GSK-LSD1 KDM LSD1 no 03/14
LLY-507 Histone Methyltransferase SMYD2 SGC705 no 11/13
PFI-3 Bromodomains SMARCA,PB1 BDF25488524 no 11/13
A-366 Histone Methyltransferase G9a, GLP no 06/13
UNC1999 Histone Methyltransferase EZH2 UNC2400 yes 05/13
PFI-2 Histone Methyltransferase SETD7 (S)-PFI-2 no 05/13
SGC-CBP30 Bromodomains CREBBP, EP300 BDOIA513 no 03/13
I-CBP112 Bromodomains CREBBP, EP300 no 03/13
Bromosporine Bromodomains pan-Bromodomain no 01/13
UNC1215 Methyl Lysine Binder L3MBTL3 UNC1079 no 08/12
SGC0946 Histone Methyltransferase DOT1L SGC0649 no 08/12
UNC0642 Histone Methyltransferase G9a, GLP yes 08/12
GSK343 Histone Methyltransferase EZH2 no 08/12
IOX2 2OG PHD2 no 02/12
IOX1 KDM pan-2-OG no 01/12
PFI-1 Bromodomains BRD2, BRD3, BRD4, BRDT (BET) no 11/11
UNC0638 Histone Methyltransferase G9a, GLP UNC0737 no 06/10
JQ1 Bromodomains BRD2, BRD3, BRD4, BRDT (BET) (-)-JQ1 yes 06/10
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