||Diflunisal is a cyclooxygenase (COX) Inhibitor, used as an anti-inflammatory analgesic.
||BET-IN-2 is a BET inhibitor (IC50: 52 nM for BRD4-BD1).
||BET-IN-4 is a potent BRD4 inhibitor (IC50 ≤ 1 μM).
||BET-IN-6 is an effective and high-affinity inhibitor of BRD2/BRD4. It is the ligand for target protein BRD2/4 and is used for the synthesis of PROTAC BRD2/BRD4 degrader-1.
||C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
||CBP/EP300-IN-2 is an inhibitor of CBP/EP300 (IC50s: 1.07 nM and 5.96 nM for CBP/HTRF and Myc) extracted from patent WO2017205538A1 (example 25).
||CBP-IN-1 is a potent inhibitor of p300/CBP bromodomain.
||CF53 is a highly potent, selective, and orally active inhibitor of BET protein (Ki: <1 nM, Kd: 2.2 nM, IC50: 2 nM for BRD4 BD1).
||CPI-0610 carboxylic acid
||CPI-0610 carboxylic acid is a ligand for target protein for PROTAC. It is a potent bromodomain and extra-terminal (BET) protein inhibitor with the potential in the therapy of multi
||E-7386 is an oral active CBP/ -catenin modulator.
||FKBP12 PROTAC dTAG-13
||FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective
||FKBP12 PROTAC dTAG-7
||FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12
||GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respective
||Histone Acetyltransferase Inhibitor II
||Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 µM).with anti-acetylase activity in mammalian cells.
||IACS-9571 is a selective and potent inhibitor of TRIM24 and BRPF1, (IC50: 8 nM for TRIM24; Kds: 31 nM and 14 nM for TRIM24 and BRPF1).
||IACS-9571 Hydrochloride is a selective and potent inhibitor of TRIM24 and BRPF1, (IC50: 8 nM for TRIM24; Kds: 31 nM and 14 nM for TRIM24 and BRPF1).
||LT052 shows nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2. LT052 has inhibitory activities against BRPF1b (IC50=567.5 nM). LT052 has anti-inflammatory activity.
||MS402 is a novel BD1-selective BET BrD inhibitor.
||MS645 is an inhibitor of bivalent BET bromodomains (BrD) (Ki of 18.4 nM for BRD4-BD1/BD2).
||OXFBD04 is a potent and selective inhibitor of BRD4(IC50 of 166 nM).
||P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).
||PNZ5 is a potent and isoxazole-based pan-BET inhibitor, with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).
||PROTAC BRD9 Degrader-1
||PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM.
||(Rac)-BAY1238097 is a inhibitor of BET(IC50 of 1.02 μM for BRD4),used in cancer research.
||BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different MM (multiple myeloma) and AML (acute myeloid leuke
||(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
||I-BET762 carboxylic acid
||I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).
||TD-428 is a highly specific degrader of BRD4(DC50 of 0.32 nM). TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficien
||TP-472 is a selective inhibitor of BRD9 (Kd: 33 nM).
||YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific BCRP inhibitor.
||Zinc Protoporphyrin is an orally active and competitive inhibitor of heme oxygenase-1 (HO-1) and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2, and
||ZINC03129319 is an inhibitor of dengue virus (DENV) NS2B-NS3 protease,and has inhibition constants (Ki1) of 92 μM and Ki3 of 20 μM.
||ZM223 is a potent non-covalent inhibitor of NEDD8 activating enzyme (NAE).
||GSK9311 hydrochloride, a less active analog of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain (pIC50s: 6.0 and 4.3 for BRPF1 and BRPF2)
||GSK9311 inhibits BRPF bromodomain (pIC50: 6.0 and 4.3 for BRPF1 and BRPF2, respectively). GSK9311 is a less active analog of GSK6853. It can be used as a negative control.
||MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)
||MZP-55 is a selective BRD3/4 degrader based on PROTAC technology(Brd4BD2 with Kd of 8 nM)
||PROTAC BRD4 Degrader-1
||PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).
||PROTAC BRD4 Degrader-2
||PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).
||PROTAC BRD4 Degrader-3
||PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.
||SMARCA-BD ligand 1 for Protac
||SMARCA-BD ligand 1 for Protac is a compound capable of binding to SMARCA2, the BAF ATPase subunit, based on the Protac technology for degrading SMARCA2
||PROTAC BET Degrader-1
||PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.
||PROTAC BET degrader-3
||PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.
||SMARCA-BD ligand 1 for Protac dihydrochloride
||SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
||PROTAC BRD9-binding moiety 1
||PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
||(R)-UT-155 is a selective androgen receptor degrader (SARD) ligand.
||A-485 is a potent and selective catalytic p300/CBP inhibitor(IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively).
||BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds o
||BETd-260 is a potent degrader of BET based on PROTAC technology, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.
||BMS-986158 is a potent BET inhibitor. With IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respect
||BRD4 Inhibitor-10 is an inhibitor of BRD4-BD1 (IC50: 8 nM).
||CTPB is a p300 histone acetyltransferase (HAT) enzyme activator.
||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
||EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).
||GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
||GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excelle
||GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
||GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).
||GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).
||GSK8573 is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 (Kd of 1.04 μM).
||GSK8814 is a selective and ATAD2/2B bromodomain chemical probe and inhibitor (binding constant pKd=8.1 and a pKi=8.9 in BROMOscan). GSK8814 displays 500-fold selectivity for ATAD2
||HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2
||LUT014 is a B-Raf inhibitor (IC50: 11.7 nM) and developed to decrease dose-limiting acneiform lesions associated with EGFR Inhibitors treatment.
||MRS2698 is an effective and highly selective agonist of the P2Y2 receptor (EC50: 8 nM). MRS2698 also is >300-fold P2Y2-selective versus the P2Y4 and P2Y6 receptors.
||MS417 is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7
||TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor (Kd: 134 nM and 5.02 μM for CBP and BRD4).
||VZ185 is an effective and selective dual BRD7/9 PROTAC degrader (DC50s: 4.5 and 1.8 nM, respectively).
||ZL0454 is an effective and selective Bromodomain-containing protein 4 inhibitors (IC50: 49 and 32 nM for BD1 and BD2).
||ZXH-3-26 is a selective degrader of the PROTAC BRD4 (DC50/5h: ~ 5 nM).
||(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1(IC50 of 10.4 nM).
||MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.
||GSK 525762A (I-BET 762) is an inhibitor of BET proteins (IC50: about 35 nM).
||Zinc sulfate heptahydrate
||Zinc sulfate heptahydrate is a dietary supplement used for zinc deficiency and to prevent the condition in those at high risk.
||(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 is a BET bromodomain inhibitor, acting on BRD4(1/2)(IC50 of 77 nM/33 nM in a cell-free assay)
||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
||PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.
||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
||XD14 is an inhibitor of BET bromodomain (Kd of 160 nM, 170 nM, 380 nM, 490 nM, 830 nM and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2), respectively).
||BET bromodomain inhibitor
||BET bromodomain inhibitor is a potent BET inhibitor.
||(+)-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).
||OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain.
||INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2
||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
||UNC669 is an effective and specific MBT (malignant brain tumor) inhibitor with IC50 of 4.2/3.1 uM for L3MBTL1/3.
||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
||GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.
||CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
||C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
||RVX-208, an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.
||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.
||GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
||AZD5153 6-Hydroxy-2-naphthoic acid
||AZD5153 (6-Hydroxy-2-naphthoic Acid) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor used in cancer treatments.
||3, 6'-Disinapoyl sucrose shows the neuroprotective effect and antidepressive activity in rats.
||Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain in
||I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
||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).
||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
||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
||CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).
||FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4.
||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.
||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.
||dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
||666-15 is a potent and selective CREB inhibitor (IC50: 81 nM).
||Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).
||INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
||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
||ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectivel
||MZ 1 is a BRD4 protein degrader based on PROTAC technology.
||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
||A1874 is a nutlin-based and BRD4-degrading PROTAC which induces BRD4 degradation in cells. Effective in inhibiting many cancer cell lines proliferation.
||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)
||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 ,
||Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus. Cycloastragenol (CAG) may
||GSK1324726A is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).
||CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
||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
||BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
||PFI-1, a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.
||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.
||Anacardic Acid is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits
||SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).
||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.
||CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
||ZL0420 is a potent and selective BRD4 inhibitor. ZL0420 reduces airway inflammation and inhibits the TLR3-dependent innate immune gene program.
||I-BRD9 is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.
||PFI-3 is a selective chemical inhibitor for SMARCA (2/4) (Kd = 89 nM)and PBI (5) bromodomains which may result in the delay and prevention of breast cancer.
||CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.
||KG-501 is a cAMP response element-binding protein (CREB) inhibitor(IC50 : 6.89 μM).
||nAS-E is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.
||Hexamethylene bisacetamide inhibits BET Bromodomain Proteins.
||UNC1079 is an selective L3MBTL3 domain inhibitor
||Alobresib is an inhibitor of BET bromodomain,is an antineoplastic drug candidate.
||NEO2734 is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).
||MS7972 is CREBBP inhibitor that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM
||TTK21 is an activator of CBP/p300 histone acetyltransferase activity.
||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 sti
||NP213 is a rapidly acting synthetic antimicrobial peptide (AMP). NP213 is effective and well-tolerated in resolving nail fungal infections. NP213 has anti-fungal activities. NP213
||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
||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).