|Description||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 inhibitor may have a similar function and utility to IL-6 neutralizing antibodies, such as tocilizumab, in the treatment of rheumatoid arthritis.|
|Synonyms||N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,4-dimethyl-2-oxoquinolin-7-yl)-6-oxopiperidin-3-yl]-2-methylpropane-1-sulfonamide N-((2R,3S)-2-(4-chlorophenyl)-1-(1,4-dimethyl-2-oxo-1,2-dihydroquinolin-7-yl)-6-oxopiperidin-3-yl)-2-methylpropane-1-sulfonamide N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,4-dimethyl-2-oxo-1,2-dihydroquinolin-7-yl)-6-oxopiperidin-3-yl]-2-methylpropane-1-sulfonamide GTPL8572 LP99|
AZD5153 6-Hydroxy-2-naphthoic acid
AZD5153 6-Hydroxy-2-naphthoic acid, a 6-hydroxy-2-naphthoic acid salt of AZD-5153, is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor p...
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...
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...
Mivebresib is a BET inhibitor with potential antineoplastic activity. It disrupts critical transcription programs that drive prostate cancer growth to induce po...
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...
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= ...
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= ...
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 ...
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity.
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.
TG101209 is a novel and potent JAK2 inhibitor. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosi...
The (R) - isomer form of JQ1 which is a BET inhibitor that could probably influence the inflammatory expression at some extent.
Bromosporine, a broad spectrum inhibitor for bromodomains which play a key role in many cellular processes, is a chemical probe for bromodomain functional assay...
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...
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
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...
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), ...
BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively), with selectivity for ...