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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 of reactive oxygen species, possesses anti-inflammatory properties as a result of inhibition of cyclooxygenases (COX) an
T1854 MS436 MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.
T1906 GSK-525762A(I-BET-762) 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 bromodomains, including BRPF2/3 and BET family bromodomains.
T1973 PFI-4 PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.
T1993 J-147 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 neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated
T2072 BET bromodomain inhibitor BET bromodomain inhibitor is a potent BET inhibitor.
T2091 CPI-0610 CPI-0610 is an effective, specific, and cell-active BET bromodomain inhibitor CPI-0610 inhibits BRD4-BD1 (IC50: nM).
T2110 (+)-JQ-1 (+)-JQ1, a BET bromodomain inhibitor, binds to all bromodomains of the BET family.
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 UNC 669 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 members of the human MBT family.
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 RVX-208 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 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, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myelo
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 inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preven
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 dose-dependently inhibits the L3MBTL13xMBT-H4K20me1 interaction. UNC-926 has not an effect on the binding of 53BP1 to H4
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 bromodomains. I-CBP112 significantly reduced the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cel
T6021 GSK1324726A (I-BET726) 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 OTX015 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 activity.
T6222 PFI-1 (PF-6405761) 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 prostaglandin synthase, lipoxygenase, and tyrosinase.
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).
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