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Epigenetic Reader Domain
| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| 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. |
| 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. |
| CSN13057 | Apabetalone | 1044870-39-4 | RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 M. |
| 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. |
| 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. |
| CSN13300 | Naringenin triacetate | 3682-04-0 | Naringenin triacetate is a natural product isolated and purified from the fruits of Citrus aurantium L. with a better binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) when compared with the known inhibitors. |
| 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 | MS402 | 1672684-68-2 | MS402 is a domain-selective inhibitor of BRD4-BD1 with Ki value of 77nM, over BRD4-BD2. |
| CSN50391 | Inobrodib | 2222941-37-7 | Inobrodib is a potent and selective p300/CBP bromodomain inhibitor. |
| 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 | Molibresib | 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 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]. |
| CSN22308 | dBET6 | 1950634-92-0 | dBET6 is an optimized and highly cell-permeable chemical degrader of BET bromodomain proteins, based on PROTAC. |
| 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. |
| CSN21391 | BRD4 degrader AT1 | 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. |
| 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. |
| 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. |
| CSN24157 | 666-15 | 1433286-70-4 | 666-15 is a potent and selective CREB inhibitor with IC50 value of 81nM. |
| 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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