|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|
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins with potential antineoplastic activity.
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...
TG101209 is a novel and potent JAK2 inhibitor. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosi...
GSK9311 is a potent and selective inhibitor of the BRPF bromodomain (pIC50= 6.0 and 4.3 for BRPF1 and BRPF2, respectively).
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...
PF-431396 is a dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively).
Bromosporine, a broad spectrum inhibitor for bromodomains which play a key role in many cellular processes, is a chemical probe for bromodomain functional assay...
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), ...
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...
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...
MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second.
Olinone, a pyridoindol derivative, has been found to be an BET Bromodomain inhibitor and could be probably useful in sorts of biological studies.
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...
Mivebresib is a BET inhibitor with potential antineoplastic activity. It disrupts critical transcription programs that drive prostate cancer growth to induce po...
CPI-0610, a benzazepine derivative, has been found to influence tumor cell growth at some extent by acting as a BET bromodomain inhibitor. IC50: < 500 nM for BR...
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 ...
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...
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 ...