Table 1.
Epigenetic probes generated by SGC.
| Protein Family | Protein | Probe |
|---|---|---|
| Bromodomain | BET (BRD2/3/4,BRDT) | (+)-JQ1, PFI-1 |
| Bromodomain | BAZ2A/2B | GSK2801, BAZ2-ICR |
| Bromodomain | BRD9/7; BRD9 | LP99,BI-9564,TP-472; I-BRD9 |
| Bromodomain | BRPF1/2/3; BRPF1B | NI-57,OF-1; PFI-4, GSK6853 |
| Bromodomain | BRPF2/TAF1 | BAY-299 |
| Bromodomain | CECR2 | NVS-CECR2–1 |
| Bromodomain | CREBBP, EP300 | SGC-CBP30, I-CBP112 |
| Bromodomain | SMARCA2/4, PB1 | PFI-3 |
| Bromodomain | ATAD2/ATAD2B; ATAD2 | GSK8814, BAY-850 |
| Dehydrogenase | IDH1 mutant | GSK864 |
| Demethylase | JMJD3/UTX | GSK-J4 (pro-drug of GSK-J1) |
| Demethylase | LSD1 | GSK-LSD1 |
| Methyllysine binder | L3MBTL3 | UNC1215 |
| Methyllysine binder | EED | A-395 |
| Methyltransferase | DOT1L | SGC0946 |
| Methyltransferase | EZH2/H1 | GSK343, UNC1999 |
| Methyltransferase | G9a/GLP | UNC0638, A-366, UNC0642 |
| Methyltransferase | PRMT Type I | MS023 |
| Methyltransferase | PRMT3 | SGC707 |
| Methyltransferase | PRMT4/6 | MS049 |
| Methyltransferase | PRMT4 | TP-064 |
| Methyltransferase | PRMT5 | GSK591, LLY-283 |
| Methyltransferase | SETD7 | (R)-PFI-2 |
| Methyltransferase | SMYD2 | BAY-598, LLY-507* |
| Methyltransferase | SUV420H1/H2 | A-196 |
| Deiminase | PAD4 | GSK484 |
| WD Domain | WDR5 | OICR-9429 |
*
This probe has been found to have several off-target activities although it meets the criteria for a chemical probe (http://www.thesgc.org/chemical-probes/LLY-507). We recommend usage of this compound only in parallel with another SMYD2 chemical probe but not on its own.