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Cat.No. Product Name Information Product Use Citations Product Validations
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
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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
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
Inflammation, 2022, 45(3):1388-1401
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
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, 2025.08.30.673282
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
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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.
Sci Adv, 2025, 11(49):eadu2292
J Nanobiotechnology, 2024, 22(1):692
J Pathol, 2024, 262(1):37-49
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
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
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S2780 I-BET151 (GSK1210151A) I-BET151 (GSK1210151A) is a novel selective BET inhibitor that targets BRD2, BRD3, and BRD4 with respective IC50 values of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays.
Elife, 2025, 13RP103064
PLoS Pathog, 2025, 21(4):e1012467
Drug Des Devel Ther, 2025, 19:8679-8689
Verified customer review of I-BET151 (GSK1210151A)

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