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BET
BET製品
- All (65)
- BET阻害剤 (59)
- BETモジュレータ(1)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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| S7110 | (+)-JQ1 | (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
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| S1109 | BI 2536 | BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. |
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| S7360 | Birabresib (OTX015) | Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
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| S2780 | I-BET151 (GSK1210151A) | I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively. |
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| S7189 | Molibresib (I-BET-762) | Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins. |
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| S7525 | XMD8-92 | XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
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| S7295 | Apabetalone (RVX-208) | Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2. |
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| S7304 | CPI-203 | CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4. | ||
| S7315 | PFI-3 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
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| S8344 | AZD5153 6-hydroxy-2-naphthoic acid | AZD5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes. | ||
| S1216 | PFI-1 (PF-6405761) | PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay. | ||
| S8400 | Mivebresib (ABBV-075) | Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell. | ||
| S8762 | dBET6 | dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis. | ||
| S8723 | ABBV-744 | ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers. | ||
| S7835 | I-BRD9 | I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4. | ||
| S7233 | Bromosporine | Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively. | ||
| S8739 | PLX51107 | PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range). | ||
| S7620 | GSK1324726A (I-BET726) | GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. | ||
| S7853 | Pelabresib (CPI-0610) | Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. | ||
| S8297 | ARV-825 | ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC. | ||
| S8180 | PF-CBP1 HCl | PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively. | ||
| S8753 | INCB054329 | INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively. | ||
| S7305 | MS436 | MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. |
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| S8589 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. | ||
| S8889 | MZ-1 | MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2. | ||
| S8296 | dBET1 | dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment. | ||
| S8190 | CPI-637 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. | ||
| S8179 | BI-7273 | BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor. | ||
| S8714 | INCB057643 | INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones. | ||
| S0137 | dBET57 | dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. dBET57 is inactive on BRD4BD2. | ||
| S8113 | BI-9564 | BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively. | ||
| E1103 | AU-15330 | AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumor growth in xenograft models of prostate cancer. | ||
| S8961 | Alobresib (GS-5829) | Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling. | ||
| S8785 | A1874 | A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency. | ||
| S8665 | GNE-781 | GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity. | ||
| S9691 | BMS-986158 | BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively. | ||
| E1932 | DW71177 | DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia. | ||
| E1517 | ZEN-3694 (BET-IN-19) | ZEN-3694 is an orally bioavailable bromodomain extraterminal inhibitor (BETi) that leads to down-regulation of expression of AR-signaling in metastatic castrationresistant prostate cancer (mCRPC) models. | ||
| E1926New | IBG1 | IBG1 (PROTAC BRD4 Degrader-19) is a PROTAC-like degrader specifically targeting BET bromodomains with a DC50 of 0.15 nM for BRD4. It consists of the BET inhibitor JQ1 linked to E7820 and functions through CRL4-DCAF16. | ||
| S8763 | ZL0420 | ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog. | ||
| E0494 | NI-42 | NI-42 is a biased, potent inhibitor of the of the bromodomain and PHD finger-containing (BRPF) with IC50s of 7.9, 48, 260 nM for BRPF1/2/3. | ||
| S8625 | GNE-049 | GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively. | ||
| E1095 | ODM-207 | ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models. | ||
| E4712 | SDU-071 | SDU-071 is an inhibitor of BRD4-p53 protein-protein interaction with IC50 of 2.7 μM, which suppresses MDA-MB-231 triple-negative breast cancer (TNBC) cell migration, invasion, and in vivo tumor growth. It also exhibits antiproliferative activity in concentration concentration-dependent manner, with IC50 of 10.5 μM (72 h) and 12.6 μM (96 h) in MDA-MB-231 cells. | ||
| S1027 | FL-411 | FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction. | ||
| S0344 | Y06036 | Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM. | ||
| E1859 | FHD-609 | FHD-609 acts as a selective inhibitor and degrader of BRD9 protein (bromodomain-containing protein 9). FHD-609 targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit. | ||
| S8948 | SRX3207 | SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. | ||
| S7615 | MS417 | MS417 (GTPL7512) is a selective inhibitor of BET-specific BRD4. MS417 binds to BRD4-BD1 and BRD4-BD2 with IC50 values of 30 nM and 46 nM and Kd values of 36.1 nM, and 25.4 nM, respectively. MS417 effectively blocks BRD4 binding to the acetylated NF-κB and attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα. | ||
| S3573 | Trotabresib (CC-90010) | Trotabresib (CC-90010) is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors. | ||
| E1144 | dBRD9 | dBRD9 is a bifunctional molecule that links a small molecule that specifically binds to the bromodomain of BRD9 and another ligand that recruits the cereblon E3 ubiquitin ligase, potently and selectively degrades BRD9 with IC50 of 104 nM in MOLM-13 cells. | ||
| E0807 | NHWD-870 | NHWD-870 inhibits CSF1 expression through suppressing BRD4 and its target HIF1α. | ||
| E1664 | GNE-987 | GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. GNE-987 inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines. | ||
| S2941 | (+)-JQ1 PA | (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1. | ||
| E4609 | Amredobresib | Amredobresib (BI894999) is an oral inhibitor of BET, which acts as an acetyl-lysine mimic. It prevents the bromodomains BRD4-BD1 and BRD4-BD2 from binding to acetylated histones, with an IC50 of 5 nM for BRD4-BD1 and 41 nM for BRD4-BD2. | ||
| S8574 | BRD4 Inhibitor-10 | BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM. | ||
| S8545 | TEN-010 ((S)-JQ-35) | TEN-010 (RG6146, Ro-6870810,(S)-JQ-35) is an inhibitor of the Bromodomain and Extra-Terminal(BET) family bromodomain-containing proteins with potential antineoplastic activity. | ||
| E8018 | BAY-299 | BAY-299 is a potent dual inhibitor that targets the bromodomain and PHD finger (BRPF) family member BRPF2, along with the TATA box binding protein-associated factors TAF1 and TAF1L, with an IC50 of 67 nM for BRPF2 BD, 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2. | ||
| E1177 | CFT8634 | CFT8634 is a potent BRD9 degrader with DC50 of 3 nM. It forms a ternary complex with BRD9 and an E3 ligase, resulting in BRD9 ubiquitination. CFT8634 is used in the treatment of SMARCB1-perturbed cancers. | ||
| S9683 | GSK778 (iBET-BD1) | GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. | ||
| S6397 | Thalidomide-NH-C4-NH-Boc | Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers. | ||
| S9684 | GSK046 (iBET-BD2) | GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity. | ||
| S9685 | GSK620 | GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics. | ||
| E4713 | BBC0403 | BBC0403 is a small-molecule selective inhibitor of Bromodomain-containing protein 2(BRD2) with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. It is a potential intra-articular injectable therapeutic agent for treating osteoarthritis (OA). | ||
| E0781 | BAZ1A-IN-1 | BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein), exerting a Kd value of 0.52 μM against BAZ1A bromodomain, shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A. | ||
| S7110 | (+)-JQ1 | (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
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| S1109 | BI 2536 | BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. |
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| S7360 | Birabresib (OTX015) | Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
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| S2780 | I-BET151 (GSK1210151A) | I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively. |
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| S7189 | Molibresib (I-BET-762) | Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins. |
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| S7525 | XMD8-92 | XMD8-92 is a potent and selective dual inhibitor of big map kinase (BMK1, ERK5) and bromodomain-containing proteins (BRDs, BET) with Kd of 80 nM and 170 nM for ERK5 and BRD4(1), respectively. |
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| S7295 | Apabetalone (RVX-208) | Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2. |
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| S7304 | CPI-203 | CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4. | ||
| S8344 | AZD5153 6-hydroxy-2-naphthoic acid | AZD5153 6-hydroxy-2-naphthoic acid (HNT salt) is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with pKi of 8.3 for BRD4. AZD5153 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. NSD3, via H3K36me2, acts as an epigenetic deregulator to facilitate the expression of oncogenesis-promoting genes. | ||
| S1216 | PFI-1 (PF-6405761) | PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay. | ||
| S8400 | Mivebresib (ABBV-075) | Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell. | ||
| S8762 | dBET6 | dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis. | ||
| S8723 | ABBV-744 | ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. It is developed for treating AML and cancers. | ||
| S7835 | I-BRD9 | I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4. | ||
| S7233 | Bromosporine | Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively. | ||
| S8739 | PLX51107 | PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range). | ||
| S7620 | GSK1324726A (I-BET726) | GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. | ||
| S7853 | Pelabresib (CPI-0610) | Pelabresib (CPI-0610) is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with an IC50 of 39 nM for BRD4-BD1 in TR-FRET assay and currently undergoing human clinical trials for hematological malignancies. CPI-0610 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. | ||
| S8180 | PF-CBP1 HCl | PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively. | ||
| S8753 | INCB054329 | INCB054329 is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively. | ||
| S7305 | MS436 | MS436 is a selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. |
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| S8589 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. | ||
| S8296 | dBET1 | dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment. | ||
| S8190 | CPI-637 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor. | ||
| S8179 | BI-7273 | BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor. | ||
| S8714 | INCB057643 | INCB057643 is a BET inhibitor that binds to the acetylated lysine recognition motifs found in the BRD of BET proteins, thereby preventing the interaction between the BET proteins and acetylated lysines on histones. | ||
| S0137 | dBET57 | dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. dBET57 is inactive on BRD4BD2. | ||
| S8113 | BI-9564 | BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains with the IC50 of 75 nM and 3.4 µM, respectively. | ||
| E1103 | AU-15330 | AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumor growth in xenograft models of prostate cancer. | ||
| S8961 | Alobresib (GS-5829) | Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling. | ||
| S8785 | A1874 | A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency. | ||
| S8665 | GNE-781 | GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity. | ||
| S9691 | BMS-986158 | BMS-986158 is a potent inhibitor of BET with IC50s of 6.6 nM and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively. | ||
| E1932 | DW71177 | DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia. | ||
| E1517 | ZEN-3694 (BET-IN-19) | ZEN-3694 is an orally bioavailable bromodomain extraterminal inhibitor (BETi) that leads to down-regulation of expression of AR-signaling in metastatic castrationresistant prostate cancer (mCRPC) models. | ||
| S8763 | ZL0420 | ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog. | ||
| E0494 | NI-42 | NI-42 is a biased, potent inhibitor of the of the bromodomain and PHD finger-containing (BRPF) with IC50s of 7.9, 48, 260 nM for BRPF1/2/3. | ||
| S8625 | GNE-049 | GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively. | ||
| E1095 | ODM-207 | ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. ODM-207 also shows potent antiproliferative effects in patient-derived cancer cells and in xenograft models. | ||
| E4712 | SDU-071 | SDU-071 is an inhibitor of BRD4-p53 protein-protein interaction with IC50 of 2.7 μM, which suppresses MDA-MB-231 triple-negative breast cancer (TNBC) cell migration, invasion, and in vivo tumor growth. It also exhibits antiproliferative activity in concentration concentration-dependent manner, with IC50 of 10.5 μM (72 h) and 12.6 μM (96 h) in MDA-MB-231 cells. | ||
| S1027 | FL-411 | FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction. | ||
| S0344 | Y06036 | Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM. | ||
| E1859 | FHD-609 | FHD-609 acts as a selective inhibitor and degrader of BRD9 protein (bromodomain-containing protein 9). FHD-609 targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit. | ||
| S8948 | SRX3207 | SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. | ||
| S7615 | MS417 | MS417 (GTPL7512) is a selective inhibitor of BET-specific BRD4. MS417 binds to BRD4-BD1 and BRD4-BD2 with IC50 values of 30 nM and 46 nM and Kd values of 36.1 nM, and 25.4 nM, respectively. MS417 effectively blocks BRD4 binding to the acetylated NF-κB and attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα. | ||
| S3573 | Trotabresib (CC-90010) | Trotabresib (CC-90010) is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors. | ||
| E1144 | dBRD9 | dBRD9 is a bifunctional molecule that links a small molecule that specifically binds to the bromodomain of BRD9 and another ligand that recruits the cereblon E3 ubiquitin ligase, potently and selectively degrades BRD9 with IC50 of 104 nM in MOLM-13 cells. | ||
| E0807 | NHWD-870 | NHWD-870 inhibits CSF1 expression through suppressing BRD4 and its target HIF1α. | ||
| S2941 | (+)-JQ1 PA | (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1. | ||
| E4609 | Amredobresib | Amredobresib (BI894999) is an oral inhibitor of BET, which acts as an acetyl-lysine mimic. It prevents the bromodomains BRD4-BD1 and BRD4-BD2 from binding to acetylated histones, with an IC50 of 5 nM for BRD4-BD1 and 41 nM for BRD4-BD2. | ||
| S8574 | BRD4 Inhibitor-10 | BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM. | ||
| S8545 | TEN-010 ((S)-JQ-35) | TEN-010 (RG6146, Ro-6870810,(S)-JQ-35) is an inhibitor of the Bromodomain and Extra-Terminal(BET) family bromodomain-containing proteins with potential antineoplastic activity. | ||
| E8018 | BAY-299 | BAY-299 is a potent dual inhibitor that targets the bromodomain and PHD finger (BRPF) family member BRPF2, along with the TATA box binding protein-associated factors TAF1 and TAF1L, with an IC50 of 67 nM for BRPF2 BD, 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2. | ||
| S9683 | GSK778 (iBET-BD1) | GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. | ||
| S6397 | Thalidomide-NH-C4-NH-Boc | Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers. | ||
| S9684 | GSK046 (iBET-BD2) | GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity. | ||
| S9685 | GSK620 | GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics. | ||
| E4713 | BBC0403 | BBC0403 is a small-molecule selective inhibitor of Bromodomain-containing protein 2(BRD2) with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. It is a potential intra-articular injectable therapeutic agent for treating osteoarthritis (OA). | ||
| E0781 | BAZ1A-IN-1 | BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein), exerting a Kd value of 0.52 μM against BAZ1A bromodomain, shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A. | ||
| S8889 | MZ-1 | MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2BD1, Brd2BD2, Brd3BD1, Brd3BD2, Brd4BD1 and Brd4BD2. | ||
| E1926New | IBG1 | IBG1 (PROTAC BRD4 Degrader-19) is a PROTAC-like degrader specifically targeting BET bromodomains with a DC50 of 0.15 nM for BRD4. It consists of the BET inhibitor JQ1 linked to E7820 and functions through CRL4-DCAF16. |
BETシグナル伝達経路
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間