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Bromodomain BET/PROTAC

货号 产品名 CAS号 信息
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.
CSN22296 QCA570 2207569-08-0 QCA570 is a potent PROTAC targeting on BET, consist of an optimized BET ligand QCA276 linked to a CRBN E3 ligand.
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.
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].
CSN22195 PROTAC BET Degrader-1 2093386-22-0 PROTAC BET degrader-9 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and Pomalidomide as CRBN ligand.
CSN24002 PROTAC BET degrader-3 N/A PROTAC BET degrader-3 is PROTAC targeting on BET proteins.
CSN23933 PROTAC BET degrader-2 2093388-33-9 PROTAC BET degrader-25 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and a Lenalidomide analogue as the CRBN ligand.
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.
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.
CSN22292 MZ 1 1797406-69-9 MZ1 is a PROTAC with VHL-ligand and targeting on BRD protein, with preferential selectivity to BRD4 (Kd=149nM) over BRD2 and BRD3.
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).
CSN22289 dBRD9 2170679-45-3 dBRD9 is a potent and selective PROTAC targeting on BRD9, with a PEG-linked pomalidomide
CSN23970 dBRD9 2HCl 2341840-98-8 dBRD9 is a potent and selective PROTAC targeting on BRD9, with a PEG-linked pomalidomide
CSN22308 dBET6 1950634-92-0 dBET6 is an optimized and highly cell-permeable chemical degrader of BET bromodomain proteins, based on PROTAC.
CSN22286 dBET1 1799711-21-9 dBET1 is a PROTAC, consisting of a BRD4-ligand JQ-1 linkerd to a cereblon E3 ligase ligand, targeting on BET bromodomain BRD4
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).
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.
CSN22293 ARV-771 1949837-12-0 ARV-771 is a PROTAC targeting on pan-BET, containing a BRD4-binding moiety (JQ-1) and a VHL-binding moiety.
CSN23919 A1874 2064292-12-0 A1874 is a nutlin-based PROTAC targeting on BRD4, consist of a BRD4-ligand JQ1 linked to a MDM2 E3 ligase ligand RG7388.
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