| DC49605 |
CREB-IN-1 TFA |
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth. |
|
| DC70972 |
MI-1 |
MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM. |
|
| DC71230 |
SDR-04 |
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation. |
|
| DC71319 |
OXFBD02 |
OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50
value of 382 nM. |
|
| DC71320 |
(2S,3R)-LP99 |
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion. |
|
| DC71321 |
ET-JQ1-OH
Featured
|
ET-JQ1-OH is an allele-specific BET inhibitor. |
|
| DC71503 |
PROTAC_ERRα |
PROTAC_ERRα is a potent and selective ERRα degrader. PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. |
|
| DC71504 |
Thalidomide-NH-C4-NH-Boc |
Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers. |
|
| DC71746 |
QA-68 |
QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines. |
|
| DC72030 |
GNE-064
Featured
|
GNE-064 (compound 5) is a selective, oral and highly soluble inhibitor of the SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis. |
|
| DC72179 |
UNC1021
Featured
|
UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM. |
|
| DC72325 |
I-BET432 |
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases. |
|
| DC72610 |
Physachenolide C |
Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity. |
|
