|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|
I-BET151, also known as GSK1210151A, is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. I-BET151 (GSK1210151A) shows good oral b...
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 ...
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
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= ...
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...
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 ...
TG101209 is a novel and potent JAK2 inhibitor. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosi...
MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second.
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.
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...
BET-IN-1, an oxazole derivative, can be used as a bromodomain inhibitor
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...
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...
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 ...
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...
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.
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...
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...
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, ...