Chemical Probes


Identification of fragments that displace histone peptides from bromodomains

Chemical Probes

Potent, selective and cell-permeable inhibitors of protein function ("chemical probes") are valued reagents in both fundamental and applied biological research, and they are essential for the early stages of drug discovery by allowing preclinical target validation in both academic and industrial laboratories.

SGC chemical probes meet the following criteria:

  • In vitro potency of <100 nM
  • >30-fold selectivity vs other subfamilies
  • Demonstration of on-target effect in cells at <1 µM
 

 

 

Probe dissemination

Every SGC probe is accompanied by a web resource containing relevant information

  • Physical/ Chemical Properties
  • Selectivity Profile
  • Cell Based Assay Data
  • References
  • Co-crystal structures

SGC chemical probes are open-access reagents that are meant to be used by  the biomedical research community with no restrictions on use. To acquire a sample, follow the links on the webpage of your desired chemical probe. You can sort the table by clicking the column headers.

The SGC also shares cell-active broad spectrum inhibitors of a specific epigenetic target family. These are the pan-bromodomain inhibitor, bromosporine, and the pan-demethylase inhibitor, IOX-1.

Name Structure Protein Family Specific Targets Control In vivo parameters tested* Addedsort ascending
LLY-283 Methyltransferase PRMT5 LLY-284 07/16
A-395 Methyl Lysine Binder EED A-395N 07/16
BAY-876 glucose transporter GLUT1 BAY-588 06/16
TP-472 Bromodomains BRD9, BRD7 TP-472N 06/16
TP-064 Methyltransferase PRMT4 TP-064N 06/16
T-26c matrix metalloproteinase MMP-13 T-26f 06/16
BAY-299 Bromodomains BRD1, TAF1 BAY-299N 06/16
NVS-PAK1-1 Kinase PAK1 NVS-PAK1-C no 06/16
GSK864 Dehydrogenase Mutant isocitrate dehydrogenase 1 GSK990 yes 11/15
BAY-678 Serine Proteases Neutrophil Elastase BAY-677 yes 10/15
A-196 Methyltransferase SUV420H1/H2 A-197, SGC2043 no 07/15
GSK591 Methyltransferase PRMT5 SGC2096 no 07/15
MS023 Methyltransferase Type I PRMTs MS094 no 07/15
MS049 Methyltransferase PRMT4,6 MS049N 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 Methyltransferase SMYD2 BAY-369 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 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 Methyltransferase SMYD2 SGC705 no 11/13
PFI-3 Bromodomains SMARCA,PB1 BDF25488524 no 11/13
A-366 Methyltransferase G9a, GLP no 06/13
UNC1999 Methyltransferase EZH2 UNC2400 yes 05/13
PFI-2 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 Methyltransferase DOT1L SGC0649 no 08/12
UNC0642 Methyltransferase G9a, GLP yes 08/12
GSK343 Methyltransferase EZH2 no 08/12
GSKJ1 KDM JMJD3, UTX, JARID1B GSK-J2/J5 no 07/12
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 Methyltransferase G9a, GLP UNC0737 no 06/10
JQ1 Bromodomains BRD2, BRD3, BRD4, BRDT (BET) (-)-JQ1 yes 06/10
glqxz9283 sfy39587stf02 mnesdcuix8
sfy39587stf03