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| 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 | 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. |
| 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). |
| CSN67937 | NHWD-870 | 2115742-03-3 | NHWD-870 is a potent and selective BET inhibitor that targets the bromodomains of BRD2/3/4 with IC50 values of 2.7nM, as well as BRDT. |
| 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]. |
| 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 |
