|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).|
I-BRD9, as a selective cell active chemical probe for BRD9 (pIC50 = 7.3), it exhibits 200-fold selectivity for bromodomain containing protein 9 over the highly ...
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...
JQ-1, a selective BET bromodomain inhibitor with antiproliferative activity, is highly active against human leukemia OCI-AML3 mutation lines such as nucleophosm...
The (R) - isomer form of JQ1 which is a BET inhibitor that could probably influence the inflammatory expression at some extent.
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), ...
TC AC 28
TC AC 28 is a high affinity BET bromodomain ligand (Kd = 40 and 800 nM for Brd2(2) and Brd2(1), respectively) with 20-fold selectively for the second over the f...
GSK6853 is a potent (pKd 9.5), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain with greater than 1600-fold selectivity ov...
Bromosporine, a broad spectrum inhibitor for bromodomains which play a key role in many cellular processes, is a chemical probe for bromodomain functional assay...
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...
GSK9311 is a potent and selective inhibitor of the BRPF bromodomain (pIC50= 6.0 and 4.3 for BRPF1 and BRPF2, respectively).
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity.
TG101209 is a novel and potent JAK2 inhibitor. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosi...
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
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).
I-BET 151 dihydrochloride
The hydrochloride salt form of I-BET 151, which has been found to be a BET bromodomain inhibitor and exhibit activities against human and murine MLL-fusion leuk...
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= ...
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...
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...