||RVX-208, an effective BET bromodomain inhibitor,has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.
||J147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurog
||SF2523 is a highly selective and potent inhibitor.
||UNC 926 hydrochloride
||UNC-926 inhibits L3MBTL1 (IC50: 3.9 μM). UNC-926 also exhibits a low micromolar affinity for L3MBTL3. UNC-926 inhibits binding of the 3xMBT domain to H4K20me1. It selectively and
||GSK 525762A (I-BET 762) is an inhibitor of BET proteins (IC50: about 35 nM).
||(+)-JQ1 is a BET bromodomain inhibitor (IC50: 77 nM/33 nM for BRD4 (1/2)).
||I-BET151 (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).
||GSK1324726A is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).
||YF-2 is blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, CBP, PCAF, and GCN5 with EC50s of 2.75 μM, 29.04 μM and 49.31 μM , r
||UNC669 is an effective and specific MBT (malignant brain tumor) inhibitor with IC50 of 4.2/3.1 uM for L3MBTL1/3.
||MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.
||3,6'-Disinapoyl sucrose shows the neuroprotective effect and antidepressive activity in rats.
||PFI-1, a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.
||UNC1215, an effective and specific MBT (malignant brain tumor) antagonist, binds L3MBTL3 (IC50/Kd: 40/120 nM). The selectivity of UNC1215 for L3MBTL3 is 50-fold higher versus other
||666-15 is a potent and selective CREB inhibitor (IC50: 81 nM).
||Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain in
||CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
||BET bromodomain inhibitor
||BET bromodomain inhibitor is a potent BET inhibitor.
||SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).
||GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.
||Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.
||PLX51107 is a potent and selective BET inhibitor (Kds: 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1).
||I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
||Anacardic Acid is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits
||I-BRD9 is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.
||dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis.
||ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of
||A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
||INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
||KG-501 is a cAMP response element-binding protein (CREB) inhibitor(IC50 : 6.89 μM).
||Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).
||AZD5153 6-Hydroxy-2-naphthoic acid
||AZD 5153 is an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). It can simultaneously bind two bromodomains in BRD4, wh
||BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.
||BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 μM.
||NI-57 is an inhibitor of proteins of bromodomain and plant homeodomain finger-containing (BRPF) family, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respecti
||dBET57 is heterobifunctional degrader of BRD4 based on the PROTAC technology, exhibits significant degradation of BRD4BD1 with a DC50/5h of 500 nM ,and inactive on BRD4BD2
||CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
||GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
||dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
||PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).
||Birabresib is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic a
||CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
||JQ-1 carboxylic acid
||JQ-1 carboxylic acid is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)
||PF-CBP1 is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
||FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4.
||ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.
||ZL0420 is a potent and selective BRD4 inhibitor. ZL0420 reduces airway inflammation and inhibits the TLR3-dependent innate immune gene program.
||Diflunisal is a cyclooxygenase (COX) Inhibitor， used as an anti-inflammatory analgesic.
||Bisdemethoxycurcumin (BDMC) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α,25-dihydroxy vitamin D3 to stim
||Hexamethylene bisacetamide inhibits BET Bromodomain Proteins.
||C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
||CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).
||Curcumin is a phytopolylphenol pigment isolated from the plant Curcuma longa, commonly known as turmeric, with a variety of pharmacologic properties. Curcumin blocks the formation
||BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
||Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus.Cycloastragenol (CAG) may h
||ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the rela
||PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.
||GSK-5959 is an effective, specific and cell permeable BRPF1 bromodomain inhibitor (IC50: ~80 nM). The selectivity of GSK-5959 for BRPF1 is >100-fold over a panel of 35 other bromod
||OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain.
||nAS-E is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.
||I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300
||CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.