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Epigenetic Reader Domain

Epigenetic Reader Domain

货号 产品名 CAS号 信息
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 (DC50/5h=5 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 (E/Z)-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.
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.
CSN22516 PROTAC BRD9-binding moiety 1 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/β-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.
CSN27604 MS402 1672684-68-2 MS402 is a domain-selective inhibitor of BRD4-BD1 with Ki value of 77nM, over BRD4-BD2.
CSN21386 L-Moses 2079885-05-3 L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.
CSN22252 KG-501 18228-17-6 KG-501 is histochemical substrate of alkaline phosphatases and can inhibit CREB-CBP interaction.
CSN50391 Inobrodib 2222941-37-7 Inobrodib is a potent and selective p300/CBP bromodomain inhibitor.
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.
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 hydrochloride 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 (Kd=2.8 μM).
CSN21184 FL-411 2118944-88-8 FL-411 selectively inhibits BRD4 with an IC50 of 0.43 ± 0.09 μM.
CSN22308 dBET6 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 (DC50/5h=500 nM), but is inactive on BRD4 BD2.
CSN22301 dBET23 1957234-83-1 dBET23 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=50 nM) in cellular degradation assays.
CSN24814 BRD4-IN-3 1380087-86-4 CPI-268456 is a ligand of BRD4.
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.
CSN27738 CBP/p300-IN-1 2443789-32-8 CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.
CSN43576 BRD4 Inhibitor-10 1660117-38-3 BI-894999 is a potent and selective BET inhibitor that may treat hematological malignancies by inhibiting super-enhancer-driven oncogenes.
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.
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].
CSN20607 AZD5153 6-Hydroxy-2-naphthoic acid 1869912-40-2 AZD5153 is an inhibitor of BET/BRD4 bromodomain, the IC50 for BRD4 is 1.7 nM.
CSN21392 AT6 2098836-50-9 AT6 is a PROTAC targeting on Brd4.
CSN21391 BRD4 degrader AT1 2098836-45-2 AT1 is a highly selective Brd4 degrader with a modified VHL ligand retained binding to VHL (Kd = 330 nM).
CSN21253 MAK683 1951408-58-4 An inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity.
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.
CSN24157 666-15 1433286-70-4 666-15 is a potent and cell-permeable inhibitor of cAMP-response element binding protein (CREB) with efficacious anti-cancer activity both in vitro and in vivo.
CSN42118 EEDi-5273 2585648-55-9
CSN42809 Bromopropylate 18181-80-1
CSN61928 MS33 2407449-11-8
CSN80017 CFT8634 2704617-95-6
CSN104893 Dimethyl 2-hydroxy-2,3-dihydrobenzofuran-4,6-dicarboxylate 1268024-07-2
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