|Description||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), and BRD4 (IC50= 22 nM).|
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).
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), ...
OTX015 a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD). BRDs 2, 3, and 4 are considered potential cancer target...
LP99 is the first selective BRD7/9 bromodomain inhibitor. The effect of LP99 on IL-6 expression demonstrates for the first time that a small-molecule BRD7/9 in...
GSK2801 is a A Selective Chemical Probe for BAZ2B/A bromodomains. BAZ2A/B belong to a family of ubiquitously expressed bromodomain containing proteins.probes/GS...
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= ...
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= ...
CPI-0610, a benzazepine derivative, has been found to influence tumor cell growth at some extent by acting as a BET bromodomain inhibitor. IC50: < 500 nM for 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...
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).
The (R) - isomer form of JQ1 which is a BET inhibitor that could probably influence the inflammatory expression at some extent.
JQ-1, a selective BET bromodomain inhibitor with antiproliferative activity, is highly active against human leukemia OCI-AML3 mutation lines such as nucleophosm...
BET-IN-1, an oxazole derivative, can be used as a bromodomain inhibitor
OF-1 is the potent and selective BRPF (BRomodomain and PHD Finger containing) inhibitor with Kd values 100 nM, 500 nM, and 2.4 μM for BRPF1B, BRPF2, and BRPF3, ...
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
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 ...
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.
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...