Drug Class Detail

Drug Class BET Inhibitor (Pan)

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Drug Name Trade Name Synonyms Drug Classes Drug Description
INCB054329 BET Inhibitor (Pan) 25 INCB054329 is BET inhibitor, which inhibits cell proliferation (Proceedings of the 106th Annual Meeting of the AACR; 2015; Abstract nr 3525).
GS-5829 BET Inhibitor (Pan) 25 GS-5829 is a BET bromodomain inhibitor, potentially resulting in inhibition of cell growth and apoptotic activity (Blood 2016 128:5104).
TEN-010 RG-6146|JQ2|RO6870810|RG6146 BET Inhibitor (Pan) 25 TEN-010 binds to the bromodomain of BET proteins preventing their interaction with acetylated histone peptides, thus disrupting chromatin remodeling, gene expression, and cell proliferation (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr A49).
NEO2734 BET Inhibitor (Pan) 25 NEO 2734 is a dual inhibitor of the BET and CBP/P300 that demonstrates anti-tumor activities (Ann Oncol, 29(suppl_8), Oct 2018, abstract 429P).
MS436 BET Inhibitor (Pan) 25 MS436 is a BET bromodomain inhibitor with specificity for BRD4, which may result in cell cycle arrest thereby inhibiting cell proliferation (PMID: 23950209, PMID: 24144283).
JQ1 BET Inhibitor (Pan) 25 JQ1 is a BET bromodomain inhibitor with greatest specificity towards BRD4, resulting in decreased Myc expression and cell death (PMID: 24231268).
PLX51107 BET Inhibitor (Pan) 25 PLX51107 is a small molecule BET inhibitor, which binds to BET bromodomains in BRD2, BRD3, BRD4, and BRDT, potentially resulting in decreased tumor cell proliferation (PMID: 29386193).
GSK525762 Molibresib I-BET762 BET Inhibitor (Pan) 25 Molibresib (GSK525762) is a JQ1 derivative which binds to the bromodomain of BET proteins preventing their interaction with acetylated histone peptides, thus disrupting chromatin remodeling, gene expression, and cell proliferation (PMID: 24015967).
INCB057643 INCB57643 BET Inhibitor (Pan) 25 INCB057643 is an inhibitor of proteins containing BET bromodomains (Blood 2017 130:4048).
hexamethylene bisacetamide HMBA BET Inhibitor (Pan) 25 Hexamethylene bisacetamide is a polar-planar compound that inhibits BET through BD2 binding, resulting in growth inhibition and apoptosis in tumor cells (PMID: 26941288).
BMS986158 BET Inhibitor (Pan) 25 BMS986158 is BET inhibitor, which interferes with chromatin remodeling to prevent gene expression and tumor growth (NCI Drug Dictionary).
Birabresib Y-803|MK-8628|OTX015 BET Inhibitor (Pan) 25 Birabresib (OTX015) is an inhibitor of the BET bromodomain proteins BRD3, BRD4, and BRD5, which inhibits interaction with acetylated histone H4, potentially resulting in decreased tumor cell proliferation (Mol Cancer Ther Nov 2013 12:C244, PMID: 29733771).
dBET1 BET Inhibitor (Pan) 25 dBET1 is a phthalimide conjugate that targets Bet proteins for degradation, leading to growth inhibition in tumor cells (PMID: 25999370).
ODM-207 BET Inhibitor (Pan) 25 ODM-207 is a BET inhibitor that demonstrates anti-proliferative effects in tumor cells (AACR, Cancer Res: April 2016; Volume 57, Abstract #4649).
MT1 BET Inhibitor (Pan) 25 MT1 is a bivalent BET bromodomain inhibitor, which may result in tumor cell death and decreased tumor growth (PMID: 27775715).
MS417 BET Inhibitor (Pan) 25 MS417 is a BET bromodomain inhibitor with specificity for BRD4, which may result in cell cycle arrest thereby inhibiting cell proliferation (PMID: 23950209, PMID: 22645123).
RVX-208 BET Inhibitor (Pan) 25 RVX-208 is a bromo and extraterminal (BET) protein inhibitor that selectively binds to the second bromodomain found on BET proteins, resulting in inhibition of downstream gene transcription (PMID: 24248379).
ZEN003694 ZEN-3695 BET Inhibitor (Pan) 25 ZEN003694 is an inhibitor of proteins containing BET bromodomains (PMID: 27610751).
BI 894999 BET Inhibitor (Pan) 25 BI 894999 is a bromodomain (BET) inhibitor with selective activity against BRD2/3/4 and BRDT, which may result in G1 arrest and apoptosis, and inhibition of tumor growth (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr B79).
GS-626510 BET Inhibitor (Pan) 25 GS-626510 is a BET inhibitor that demonstrates anti-tumor activity (PMID: 29941483).
FT-1101 BET Inhibitor (Pan) 25 FT-1101 is a BET inhibitor capable of binding to both bromodomains in each of the four BET family members, BRD2, BRD3, BRD4, and BRDT, which may lead to inhibition of cell proliferation and tumor growth (Blood 2015 126:1367).
CPI-0610 BET Inhibitor (Pan) 25 CPI-0610 is a small molecule that binds to BET bromodomains and inhibits interaction with acetylated histones, resulting in regulation of BET-dependent gene expression and anti-tumor effects (PMID: 26815195).
BAY 1238097 BAY1238097|BAY-1238097 BET Inhibitor (Pan) 25 BAY 1238097 targets proteins of the bromodomain (BRD) and extraterminal (BET) family to prevent interaction with histones and subsequent expression of genes, such as MYC, to prevent cell growth and proliferation (PMID: 30711772).
ABBV-744 BET Inhibitor (Pan) 25 ABBV-744 is a bromodomain II selective BET inhibitor that demonstrates anti-proliferative activity (Cancer Res 2018;78(13 Suppl):Abstract nr DDT01-05).
ABBV-075 Mivebresib BET Inhibitor (Pan) 25 ABBV-075 (Mivebresib) is a bromodomain (BET) inhibitor, which may inhibit Ar and Myc downstream signalling to prevent growth and proliferation of tumor cells (PMID: 30647404).
Molecular Profile Protein Effect Treatment Approaches