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| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| CSN28527 | 17-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaheptadecyl (3R)-3-(5-amino-4-carbamoyl-3-(4-(2,4-difluorophenoxy)phenyl)-1H-pyrazol-1-yl)piperidine-1-carboxylate | 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. |
| CSN24006 | TD-428 | 2334525-50-5 | TD-428 is a PROTAC targeting on pan-BET with DC50 of 0.32nM for BRD4, consist of BET inhibitor, JQ1, as a warhead linked to CRBN modulator TD-106 as the E3 ligase ligand. |
| 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. |
