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Epigenetic Reader Domain

Epigenetic Reader Domain

Cat. No. Product Name CAS No. Information
CSN22303 ZXH-3-26 2243076-67-5 ZXH-3-26 is a BRD4 heterobifunctional small-molecule ligand PROTAC shows activity exclusively on the BRD4 BD1 DC505h5 nM and spares degradation of BRD2 or BRD3 in cellular degradation assays ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2 and BRD3
CSN23534 ZL0420   2229039-45-4 ZL0420 selectively inhibits BRD4 BD1 IC50 27 nM and BRD4 BD2 IC50 32 nM
CSN23787 YF-2 1311423-89-8 YF-2 is a highly selective and blood-brain-barrier permeable histone acetyltransferase activator, it acetylates H3 in the hippocampus.
CSN24058 Y06036 1832671-96-1 Y06036 is a potent and selective BET inhibitor with BRD4(1) bromodomain binding Kd value of 82 nM. It has antitumor activity and could be used for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).
CSN28527 XRN-82660 2250382-66-0 XRN82660, also known as BTK PROTAC 10, is a novel potent PROTAC for BTK with DC50 of 1.1 nM in cultured Ramos cells.
CSN28467 VZ185 2306193-61-1 VZ185 is a potent, fast, and selective VHL based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.
CSN16089 UNC1079 1418741-86-2 UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.
CSN22087 TPOP146 2018300-62-2 TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd of 134 nM and 5.02 μM for CBP and BRD4.
CSN13057 RVX-208   1044870-39-4 RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 M.
CSN22516 Target Protein-binding Moiety 6 2097512-23-5 PROTAC BRD9-binding moiety 1 is a I-BRD9-based warhead ligand for conjugation reactions of PROTAC targeting on BRD9.
CSN23937 PROTAC BRD9 Degrader-1 2097971-01-0 PROTAC BRD9 Degrader-1 is a PROTAC targeting on BRD9, consist of a BRD9 bromodomain probe I-BRD9 as a warhead ligand and pomalidomide as the CRBN ligand.
CSN26644 PROTAC BRD4-binding moiety 1 2101200-10-4 PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136)[1].
CSN28483 PROTAC BRD4 Degrader-7 2413382-30-4 PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively.
CSN26643 PROTAC BRD4 Degrader-5 2409538-70-9 PROTAC BRD4 Degrader-5 is a PROTAC-based BRD4 degrader. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines[1].
CSN21389 BETd-260 2093388-62-4 PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line.
CSN22491 PRI-724 1422253-38-0 PRI-724 is a selective inhibitor of the CBP-catenin interaction
CSN21058 PLX51107 1627929-55-8 PLX51107 is a potent and selective BRD4 inhibitor or BET inhibitor with novel in vitro and in vivo pharmacologic properties that emulates or exceeds the efficacy of BCR signaling agents in preclinical models of CLL.
CSN25695 NI 42 1884640-99-6 NI 42 is a selective inhibitor of BRPF with Kd values of 40, 210 and 943 nM for BRPF1B, 2 and 3, respectively. It also exhibits modest activity at BRD9 (Kd = 1130 nM).
CSN25695 NI 42 1884640-99-6 NI 42 is a selective inhibitor of BRPF with Kd values of 40, 210 and 943 nM for BRPF1B, 2 and 3, respectively. It also exhibits modest activity at BRD9 (Kd = 1130 nM).
CSN27616 NEO2734 2081072-29-7 NEO2734 is an orally dual p300/CBP and BET bromodomain inhibitor with IC50 values of <30 nM for both p300/CBP and BET bromodomains.
CSN21379 MZP-55 2010159-48-3 MZP-55 is a VHL-based PROTAC targeting on BET with pDC50/Dmax (%) values of 8.1/95, 7.5/93, 7.7/92, −/26 for Brd4 short, Brd4 long, Brd3 and Brd2 in HeLa cells, consist of I-BET726 as a warhead ligand linked to VHL ligand VH032.
CSN21378 MZP-54 2010159-47-2 MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032.
CSN17242 MS436 1395084-25-9 MS436, a diazobenzene-based small compound, is an inhibitor of BRD4 bromodomains with Ki values of 30-50 nM.
CSN27604 MS-402 1672684-68-2 MS402 is a domain-selective inhibitor of BRD4-BD1 with Ki value of 77nM, over BRD4-BD2.
CSN23256 INCB-057643 1820889-23-3 INCB057643 is an inhibitor of BET and it can reduce homologous recombination efficiency and augment PARP inhibitor activity in ovarian cancer
CSN22925 INCB054329 1628607-64-6 INCB054329 is a potent and selective BET protein inhibitor that targets BD1 and BD2 of BRD2, BRD3 and BRD4.
CSN13061 I-BET-762 1260907-17-2 I-BET 762 is an inhibitor for BET proteins with IC50 of 35 nM.
CSN28535 HJB97 2093391-24-1 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), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively).
CSN26642 GSK9311 HCl 2253733-09-2 GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively[1].
CSN22423 GSK1379725A 1802251-00-8 GSK1379725A is an inhibitor of Brd4 and a selective BPTF ligand Kd28 M
CSN22308 dBET 6 1950634-92-0 dBET6 is an optimized and highly cell-permeable chemical degrader of BET bromodomain proteins, based on PROTAC.
CSN22300 dBET57 1883863-52-2 dBET57 is a BRD4 heterobifunctional small-molecule ligand PROTAC exhibits significant and selective degradation of BRD4 BD1 DC505h500 nM but is inactive on BRD4 BD2
CSN20806 CeMMEC1 440662-09-9 CeMMEC1 is an N-methylisoquinolinone that inhibits the second bromodomain of TAF1 with Kd of 1.8 µM and IC50 of 0.9 µM.
CSN21391 AT 1 2098836-45-2 BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
CSN22309 BETd-246 2140289-17-2 BETd-246 is a second-generation BET bromodomain inhibitor. It causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
CSN24478 BET Bromodomain inhibitor 1505453-59-7 BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
CSN26641 BET bromodomain inhibitor 1 2411226-02-1 BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity[1].
CSN21392 AT6 2098836-50-9 AT6 is a PROTAC targeting on Brd4.
CSN18046 ARV-825 1818885-28-7 ARV-825 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with Kds values of 90nM and 28nM for affinity to BD1 and BD2.
CSN26166 Alobresib 1637771-14-2 Alobresib is a BET bromodomain inhibitor, a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc.
CSN21197 ABBV-744 2138861-99-9 ABBV-744 is an inhibitor of BDII-selective BET bromodomain that is being investigated to treat AML and metastic castration-resistant prostate cancer.
CSN18086 JQ-1 Carboxylic Acid 202592-23-2 (+)-JQ1 carboxylic acid is a warhead ligand with a carboxylic acid functional group for conjugation reactions of PROTAC targeting on BET.
CSN42118 EEDi-5273 2585648-55-9
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