首页AutophagyEpigenetic Reader Domain
Epigenetic Reader Domain
T0808 Diflunisal Diflunisal is a cyclooxygenase (COX) Inhibitor, used as an anti-inflammatory analgesic.
T1516 Curcumin 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
T1854 MS436 MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.
T1906 Molibresib GSK 525762A (I-BET 762) is an inhibitor of BET proteins (IC50: about 35 nM).
T1972 GSK 5959 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
T1973 PFI-4 PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.
T1993 J147 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
T2072 BET bromodomain inhibitor BET bromodomain inhibitor is a potent BET inhibitor.
T2110 (+)-JQ-1 (+)-JQ1 is a BET bromodomain inhibitor (IC50: 77 nM/33 nM for BRD4 (1/2)).
T2120 I-BET151 I-BET151 (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).
T2127 OF-1 OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain.
T2252 UNC669 UNC669 is an effective and specific MBT (malignant brain tumor) inhibitor with IC50 of 4.2/3.1 uM for L3MBTL1/3.
T2379 UNC1215 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
T2436 GSK2801 GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.
T2442 CPI-203 CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
T2452 C646 C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
T2480 Apabetalone RVX-208, an effective BET bromodomain inhibitor,has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.
T3217 PF-CBP1 hydrochloride 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.
T3311 GSK6853 GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
T3504 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
T3697 3,6'-Disinapoyl sucrose 3,6'-Disinapoyl sucrose shows the neuroprotective effect and antidepressive activity in rats.
T3712 Mivebresib Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain in
T3969 I-CBP112 I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
T3973 PF-CBP1 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).
T3986 SF2523 SF2523 is a highly selective and potent inhibitor.
T4012 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
T4247 I-CBP112 hydrochloride 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
T6021 GSK1324726A GSK1324726A is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).
T6032 Birabresib 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
T6222 PFI-1 PFI-1, a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.
T6255 Bromosporine 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.
T6668 SGC-CBP30 SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).
T6783 BI-7273 BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.
T6786 BI-9564 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.
T6811 CPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
T6859 I-BRD9 I-BRD9 is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.
T6939 PFI-3 A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
T6389 Anacardic Acid Anacardic Acid is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits
T4365 FL-411 FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4.
T4345 CeMMEC1 CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).
TL0007 Bisdemethoxycurcumin 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
T4697 ABBV-744 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.
T6026 CPI-203 CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
T5130 dBET6 dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
T4495 dBET1 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.
T6173 BI 2536 BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
T5318 666-15 666-15 is a potent and selective CREB inhibitor (IC50: 81 nM).
T5362 Y06036 Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).
T5417 INCB057643 INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
T5443 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)
T5434 ARV-825 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
T5440 Dbet57 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
T5575 Cyclogalegenol Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus.Cycloastragenol (CAG) may h
T6828 ZL0420 ZL0420 is a potent and selective BRD4 inhibitor. ZL0420 reduces airway inflammation and inhibits the TLR3-dependent innate immune gene program.
T7297 KG-501 KG-501 is a cAMP response element-binding protein (CREB) inhibitor(IC50 : 6.89 μM).
T7264 CBP/EP300-IN-1 CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.
TQ0083 NI-57 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
TQ0253 PLX51107 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).
T7856 nAS-E nAS-E is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.
T7863 Hexamethylene bisacetamide Hexamethylene bisacetamide inhibits BET Bromodomain Proteins.
T5468 YF-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 , r
T2237 ICG001 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
T12112 MS402 MS402 is an inhibitor of BD1-selective BET BrD (BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2) with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM , r
T12113 MS645 MS645 is an inhibitor of bivalent BET bromodomains (BrD) (Ki of 18.4 nM for BRD4-BD1/BD2).
T13785 MZP-54 MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)
T13786 MZP-55 MZP-55 is a selective BRD3/4 degrader based on PROTAC technology(Brd4BD2 with Kd of 8 nM)
T12338 OXFBD04 OXFBD04 is a potent and selective inhibitor of BRD4(IC50 of 166 nM).
T12346 P300/CBP-IN-5 P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).
T12513 PNZ5 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).
T13833 PROTAC BRD4 Degrader-1 PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).
T13834 PROTAC BRD4 Degrader-2 PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).
T13835 PROTAC BRD4 Degrader-3 PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.
T13848 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
T13849 PROTAC BET Degrader-1 PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.
T13850 PROTAC BET degrader-3 PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.
T12560 PROTAC BRD9 Degrader-1 PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM.
T14073 A-485 A-485 is an inhibitor of p300/CBP. For p300 and CBP histone acetyltransferase (HAT), the IC50s values are 9.8 nM and 2.6 nM, respectively.
T8453 UNC1079 UNC1079 is an selective L3MBTL3 domain inhibitor
T12660L BAY1238097 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
T14512 BAZ2-ICR 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
T14550 BETd-260 BETd-260 is a BET degrader. Which is based on PROTAC technology. With as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.
T14685 BMS-986158 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
T12660 (Rac)-BAY1238097 (Rac)-BAY1238097 is a inhibitor of BET(IC50 of 1.02 μM for BRD4),used in cancer research.
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