| DC72179 |
UNC1021
|
UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM. |
| DC71321 |
ET-JQ1-OH
|
ET-JQ1-OH is an allele-specific BET inhibitor. |
| DC48075 |
SGC-SMARCA-BRDVIII
|
SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor. |
| DC47977 |
I-BET567
|
I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation. |
| DC47894 |
SR-0813
|
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia. |
| DC46834 |
Menin-MLL inhibitor 20,MRN73473
|
Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6). |
| DC42491 |
GSK778（iBET-BD1 dihydrochloride）
|
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. |
| DC42300 |
GSK620
|
GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 |
| DC41049 |
Trotabresib (CC-90010)
|
Trotabresib (CC-90010) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. |
| DC39097 |
NEO2734
|
NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
