|Description||CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.|
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...
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...
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.
Bromosporine, a broad spectrum inhibitor for bromodomains which play a key role in many cellular processes, is a chemical probe for bromodomain functional assay...
OXF BD 02
OXF BD 02 is a first bromodomain of BRD4 inhibitor with IC50 value of 382 nM. It can reduce viability of lung adenocarcinoma cell lines and attenuate proliferat...
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= ...
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-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...
TG101209 is a novel and potent JAK2 inhibitor. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosi...
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.
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, ...
PF-CBP1, also known as PF-06670910, is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively) with more than 100-fold selectivity ...
RVX-208 is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increas...
JQ-1, a selective BET bromodomain inhibitor with antiproliferative activity, is highly active against human leukemia OCI-AML3 mutation lines such as nucleophosm...
XD 14 is a BET bromodomain inhibitor (Kd = 160, 170, 380, 490, 830 and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2) respectively). XD 14 a...
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...
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...
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...
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 ...