|Description||I-BET151, also known as GSK1210151A, is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. I-BET151 (GSK1210151A) shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.|
Mivebresib is a BET inhibitor with potential antineoplastic activity. It disrupts critical transcription programs that drive prostate cancer growth to induce po...
BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively), with selectivity for ...
GSK9311 is a potent and selective inhibitor of the BRPF bromodomain (pIC50= 6.0 and 4.3 for BRPF1 and BRPF2, respectively).
PFI-3, a potent and selective SMARCA2/4 bromodomain inhibitor, is a cell-permeable probe that binds avidly to the structurally-similar SMARCA4 bromodomain (Kd= ...
MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second.
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respect...
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity.
ARV-771, a pan-BET degrader, is a novel BET-PROTAC with superior in vivo pharmacology that recruits the E3 ligase VHL (Von Hippel-Lindau) to degrade BETPs (Kd= ...
BET bromodomain inhibitor
An BET bromodomain inhibitor can be used for the treatment of hematologic malignancies. It binds BET proteins to suppress the interaction between these proteins...
PF-431396 is a dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively).
TPOP146 is a potent and selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. TPOP146 targets the CBP br...
RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increas...
JQ-1, a selective BET bromodomain inhibitor with antiproliferative activity, is highly active against human leukemia OCI-AML3 mutation lines such as nucleophosm...
BI-2563 is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1), resulting in mitotic arr...
GSK525762A, also known as I-BET-762 and GSK525762, is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing pr...
PF-CBP1, also known as PF-06670910, is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively) with more than 100-fold selectivity ...
PF-CBP1, also known as PF-06670910, is a selective CBP/p300 bromodomain inhibitor (IC50 values are 125 and 363 nM, respectively) with >100-fold selectivity for ...
GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), ...
I-BET151, also known as GSK1210151A, is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. I-BET151 (GSK1210151A) shows good oral b...