BET Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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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. This compound is in Phase 2. |
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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. |
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| S7304 | CPI-203 | CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4. |
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| S7835 | I-BRD9 | I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with a pIC50 of 7.3, whilst this compound displayed a pIC50 of 5.3 against BRD4. |
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| S1216 | PFI-1 (PF-6405761) | PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor, and this compound shows IC50 values of 0.22 μM for BRD4 and 98 nM for BRD2 in a cell-free assay. |
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| 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. |
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| 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. |
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| 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. |
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| 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, this compound shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range). |
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| 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. |
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| 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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| S8889 | MZ-1 | MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). This compound 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. |
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| 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. |
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| 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. This compound also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. It exhibits antitumor activity. |
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| S8179 | BI-7273 | BI-7273 is a potent, selective, and cell-permeable BRD9 BD inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7 respectively in alpha assay. |
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| 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. |
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| 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 this compound and acetylated lysines on histones. |
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| S0137 | dBET57 | dBET57 is a novel, potent and selective degrader of BRD4BD1 based on the PROTAC technology with DC50/5h of 500 nM. This compound is inactive on BRD4BD2. |
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| 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. This compound is applied in the study for advanced solid tumours. |
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| 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. This compound is used in the treatment of SMARCB1-perturbed cancers. |
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| 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. |
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| S8961 | Alobresib (GS-5829) | Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutic agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. This compound inhibits CLL cell proliferation and induces leukaemia cell apoptosis through deregulation of key signalling pathways, such as BLK, AKT, ERK1/2, and MYC. It also inhibits NF-κB signalling. | ||
| E1994 | DBr-1 | DBr-1 is a DCAF1-BRD9 PROTAC, created by linking the BRD9 binder BI-956448 to the DCAF1 scaffold via a piperidine-aliphatic carbon linker. It is a potent and selective degrader of BRD9 with a DC50 of 90 nM. It overcomes intrinsic resistance to VHL-degraders, positioning DCAF1-PROTACs as a promising strategy to counter ligase-mediated resistance. | ||
| E1932 | DW71177 | DW71177 is a potent BD1-Selective inhibitor of BET. This compound selectively interacts with BD1 and exhibits strong antileukemic activity. It can also be used in the study of acute myeloid leukaemia. | ||
| E1926 | 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 bromodomain and PHD finger-containing (BRPF) with IC50s of 7.9, 48, 260 nM for BRPF1/2/3. | ||
| E1095 | ODM-207 | ODM-207 is a potent and selective BET inhibitor that is structurally unrelated to the benzodiazepine. This compound 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 tumour growth. It also exhibits antiproliferative activity in a 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). This compound induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction. | ||
| E1683 | DN02 | DN02 is a selective probe of the BRD8 bromodomain family. It exhibits potency against BRD8(1) with a Kd of 32 nM, and interestingly, demonstrated this activity to be selective over BRD8's second bromodomain (BRD8(2) with a Kd of >1000 nM) | ||
| S0344 | Y06036 | Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. This compound 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). This compound targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit. | ||
| S7615 | MS417 | MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). | ||
| 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-degrading 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. This compound 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. | ||
| S9683 | GSK778 (iBET-BD1) | GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with an 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), exhibiting immunomodulatory activity. It shows IC50 values of 264 nM, 98 nM, 49 nM, and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2, and BRDTBD2, respectively. | ||
| 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. | ||
| S1109 | BI 2536 | BI-2536 is a potent Plk1 inhibitor with an IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with a Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces Apoptosis and attenuates Autophagy. Phase 2. |
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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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| S7315 | PFI-3 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
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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. |
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| S8296 | dBET1 | dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing high 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 this compound treatment. |
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| S8190 | CPI-637 | CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9. |
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| S6993 | (+)-JQ1 carboxylic acid | (+)-JQ1 carboxylic acid ((+)-JQ1-COOH) is a (+)-JQ1 with a carboxylic acid functional group. (+)-JQ1 carboxylic acid ((+)-JQ1-COOH) can be used as a precursor to a PROTAC that targets BET bromodomains after conjugation to a linker and E3 ligase ligand. |
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| 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. |
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| 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. | ||
| 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. This compound blocks tumour immunosuppression and increases anti-tumour immunity. | ||
| S2943 | BRD9539 | BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity. |
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