|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).|
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...
ISOX DUAL is a potent inhibitor of bromodomain-containing protein 4 (BRD4), as well as the bromodomain of CREB binding protein (CBP). Its IC50 values are 1.5 an...
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...
Olinone, a pyridoindol derivative, has been found to be an BET Bromodomain inhibitor and could be probably useful in sorts of biological studies.
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 ...
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...
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.
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...
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...
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...
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= ...
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...
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...
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...
MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second.
JQ-1, a selective BET bromodomain inhibitor with antiproliferative activity, is highly active against human leukemia OCI-AML3 mutation lines such as nucleophosm...
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-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs...
TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent a...
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= ...