|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).
PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs...
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...
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...
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= ...
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...
JQ-1, a selective BET bromodomain inhibitor with antiproliferative activity, is highly active against human leukemia OCI-AML3 mutation lines such as nucleophosm...
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...
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...
I-BET151, also known as GSK1210151A, is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. I-BET151 (GSK1210151A) shows good oral bioava...
BET-BAY 002 is a potent BET inhibitor with strong in vitro and in vivo activities in AML and MM models, and with excellent pharmacokinetic properties.
Olinone, a pyridoindol derivative, has been found to be an BET Bromodomain inhibitor and could be probably useful in sorts of biological studies.
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.
BET-IN-1, an oxazole derivative, can be used as a bromodomain inhibitor
The (R) - isomer form of JQ1 which is a BET inhibitor that could probably influence the inflammatory expression at some extent.
TG101209 is a novel and potent JAK2 inhibitor. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosi...
INCB-057643 is a novel inhibitor of bromodomain and extra-terminal motif (BET) undergoing a phase I/II clinical trial for the advanced malignancy therapy. The s...
GSK 525768A is a enantiomer analogue of GSK 525762A which is a BET family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts...
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...
RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increas...