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BET Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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. It inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0379
bioRxiv, 2025, 2025.04.25.650475
Verified customer review of Birabresib (OTX015)
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.
Elife, 2025, 13RP103064
PLoS Pathog, 2025, 21(4):e1012467
Drug Des Devel Ther, 2025, 19:8679-8689
Verified customer review of I-BET151 (GSK1210151A)
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. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, and is highly selective over other bromodomain-containing proteins.
Cells, 2024, 13(13)1108
Clin Epigenetics, 2024, 16(1):185
EBioMedicine, 2023, 95:104752
Verified customer review of Molibresib (I-BET-762)
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.
Kidney Int Rep, 2025, 10(2):522-534
Clin Epigenetics, 2024, 16(1):185
Sci Adv, 2023, 9(15):eade3422
Verified customer review of Apabetalone (RVX-208)
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.
Cell Rep Med, 2025, S2666-3791(25)00384-2
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
J Immunother Cancer, 2023, 11(4)e006070
S7304 CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Cell Chem Biol, 2023, 30(8):987-998.e24
Microbiol Spectr, 2022, 10(4):e0241921
Microbiology Spectrum, 2022, e02419-21
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.
bioRxiv, 2025, 2025.03.25.645256
Cell Commun Signal, 2024, 22(1):415
Cancers (Basel), 2024, 16(6)1125
S7835 I-BRD9 I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while this compound displayed a pIC50 of 5.3 against BRD4.
Cancer Immunology Research, November 15, 2021, nan
Cancer Research Communications, January 30, 2024, 237-252
International Journal of Molecular Sciences, January 11, 2024, 905
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.
Cell Reports, September 2020, 108166
Scientific Reports, October 2025, 37099
Cancer Chemotherapy and Pharmacology, May 2022, 643-653
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.
Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120
MedComm (2020), 2022, 3(3):e152
Cell Death Dis, 2022, 13(10):912
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.
Cancer Research, 2024, 1333-1351
Clin Epigenetics, 2024, 16(1):185
American Journal of Cancer Research, 2023, 5382-5393
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.
Proceedings of the National Academy of Sciences, 2022, e2206824119
J Med Chem, 2022, 65(5):4182-4200
Front Oncol, 2022, 12:1011173
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).
J Immunol, 2025, vkaf109
Int J Mol Sci, 2023, 24(8)7623
Microbiol Spectr, 2022, 10(4):e0241921
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.
Cell Death Dis, 2024, 15(8):603
Microbiol Spectr, 2022, 10(4):e0241921
Cell, 2021, S0092-8674(21)00354-8
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.
Cell Death Dis, 2024, 15(8):603
Inflammation, 2022, 45(3):1388-1401
Mol Cancer Ther, 2021, 20(4):691-703
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.
Nature Communications, 2022, 6117
Nat Commun, 2022, 13-1:6117
Nature Aging, 2021, 165-178
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.
Cellular Physiology and Biochemistry, October 11, 2018, 640-653
Microbiology Spectrum, August 31, 2022, e0241921
Nucleic Acids Research, August 21, 2017, 8403-8410
Verified customer review of MS436
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.
Blood Cancer Discovery, 2024, 34-55
Viruses, 2024, 775
Viruses, 2024, 16(5)775
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.
bioRxiv, 2025, nan
bioRxiv, 2025, 2025.08.30.673282
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.
Translational Cancer Research, May 2020, 3354-3366
Molecular Cancer Research, July 2019, 1503-1518
Mol Cancer Res, 2019, 17(7):1503-1518
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.
Neoplasia, 2025, 70:101244
Gastroenterology, 2023, 165(1):228-243.e2
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.
Cancer Res, 2018, 78(20):5731-5740
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.
Pharmaceuticals (Basel), 2023, 16(2)199
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.
Cell Reports Medicine, 2024, 101416
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.
Sci Rep, 2023, 13(1):18554
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.
J Immunol Res, 2022, 2022:7945884
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).
Molecular Cancer Therapeutics, 2016, 1217-1226
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 tumors.
Cell Reports Medicine, March 19, 2024, 101471
Cell Reports Medicine, 2024, 101471
Cell Rep Med, 2024, 5(3):101471
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. This compound inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. It also inhibits NF-κB signaling.
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 leukemia.
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.
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 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). This compound 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. 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.
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.
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.
Nature, 2025, 10.1038/s41586-025-08721-9
Nat Commun, 2025, 16(1):4133
J Clin Invest, 2025, e177599
Verified customer review of (+)-JQ1
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.
Gut, 2025, gutjnl-2024-334274
Nat Commun, 2025, 16(1):1599
Genome Biol, 2025, 26(1):204
Verified customer review of BI 2536
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.
Stem Cell Reports, 2024, S2213-6711(24)00216-9
Mol Biol Rep, 2024, 51(1):313
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Verified customer review of XMD8-92
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.
Journal of Neuroinflammation, May 22, 2023, 119
Cell Reports, July 19, 2022, 111088
Genome Medicine, July 15, 2020, 63
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.
Proc Natl Acad Sci U S A, 2023, e2306414120
Mol Ther Nucleic Acids, 2023, 31:309-323
Cell Biol Int, 2022, 10.1002/cbin.11833
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.
bioRxiv, 2024, nan
Molecular & Cellular Proteomics, 2023, 100504
Mol Cell Proteomics, 2023, 22(3):100504
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 this compound treatment.
Experimental and Therapeutic Medicine, 2023, 12241
Exp Ther Med, 2023, 10.3892/etm.2023.12241
Exp Ther Med, 2023, 26(5):542
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.
EMBO J, 2024, 10.1038/s44318-024-00206-1
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.
Nat Genet, 2025, 57(10):2468-2481
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 tumor immunosuppression and increases anti-tumor immunity.
S2943 BRD9539 BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.