|Description||CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.|
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.
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.
RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increas...
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...
NVS-CECR2-1 is a potent and selective CECR2 (cat eye syndrome chromosome region, candidate 2) inhibitor (IC50 = 47 nM). NVS-CECR2-1 showed no cross reactivity i...
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...
Olinone, a pyridoindol derivative, has been found to be an BET Bromodomain inhibitor and could be probably useful in sorts of biological studies.
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
BET-IN-1, an oxazole derivative, can be used as a bromodomain inhibitor
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...
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...
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...
ISOX INACT is an inactive control probe of the bromodomain of CREB binding protein (CBP) PF-CBP1. It shows negligible activity at CBP and BRD4. It was used to p...
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...
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 bioava...
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 ...
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...
Bromosporine, a broad spectrum inhibitor for bromodomains which play a key role in many cellular processes, is a chemical probe for bromodomain functional assay...
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...