GSK620 (GSK-620) is a novel, potent and orally bioactive pan-BD2 (Bromodomain) inhibitor with anti-inflammatory activity.
UNC-926 is a potent and selective inhibitor of the L3MBTL1 (Lethal(3)malignant brain tumor-like protein) domain (Kd = 3.9 μM), which is a methyl-lysine (Kme) reader domain.
666-15 is a novel, cell-permeable, potent and selective inhibitor of CREB (cAMP-response element binding protein)-mediated gene transcription with IC50 of 81 nM.
TP-472 is a novel and potent BRD9/7 inhibitor (Kd = 33 and 340 nM).
SGC-CBP30 is a novel, potent and selective inhibitor of CREBBP (CBP/KAT3A) and its paralogue EP300 (KAT3B) with the potential to be used in neurodegenerative diseases (e.g. Alzheimer’s disease).
PFI-4 is a novel, potent, cell permeable and selective inhibitor of bromodomain and PHD finger-containing protein 1 (BRPF1) with antineoplastic activity.
INCB057643 is a novel, orally bioavailable BET inhibitor that has been tested in preclinical models of hematologic malignancies.
MS436 (MS-346), a diazobenzene analog, is a novel, potent and selective inhibitor of BET/BRD4 bromodomain with potential anti-inflammatory activity.
CPI-0610 (CPI0610) is a potent and selective benzoisoxazoloazepine BET (Bromodomain and Extra-Terminal) bromodomain inhibitor (IC50 = 39 nM) with anticancer effects.
GSK1324726A (I-BET726; GSK-1324726A), a tetrahydroquinoline analog, is a novel and potent ApoA1 up-regulator and selective BET Bromodomain inhibitor with anticancerand anti-inflammatory activity.