Search Result
Results for "
BRD4
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-160499
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- HY-147573
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1) .
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- HY-115926
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information .
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- HY-145909
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals .
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- HY-143235
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
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Cancer
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BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
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- HY-155078
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer .
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- HY-152209
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC50 values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer .
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- HY-160634
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- HY-146208
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
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- HY-111433
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PROTACs
Epigenetic Reader Domain
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Cancer
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BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4 BD2 in cells.
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- HY-146660
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c-Myc
Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .
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- HY-146739
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research .
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- HY-151972
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Epigenetic Reader Domain
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
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- HY-157460
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells .
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- HY-160636
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Epigenetic Reader Domain
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Others
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BRD4 Inhibitor-32 (example 15) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research .
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- HY-160660
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Epigenetic Reader Domain
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Others
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BRD4 Inhibitor-33 (example 13) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research .
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- HY-117491
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM .
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- HY-147202
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A) .
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- HY-149519
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
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- HY-142704
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Epigenetic Reader Domain
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Cancer
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BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
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- HY-142705
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Epigenetic Reader Domain
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Cancer
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BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
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- HY-RS01603
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Small Interfering RNA (siRNA)
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Others
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BRD4 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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BRD4 Human Pre-designed siRNA Set A
BRD4 Human Pre-designed siRNA Set A
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- HY-RS01604
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Small Interfering RNA (siRNA)
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Others
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Brd4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Brd4 Mouse Pre-designed siRNA Set A
Brd4 Mouse Pre-designed siRNA Set A
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- HY-RS01605
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Small Interfering RNA (siRNA)
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Others
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Brd4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brd4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Brd4 Rat Pre-designed siRNA Set A
Brd4 Rat Pre-designed siRNA Set A
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- HY-132943
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- HY-132943A
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- HY-160670
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- HY-160671
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- HY-143300
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- HY-145260
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Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
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Cancer
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BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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- HY-160672
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- HY-141843
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- HY-104072
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- HY-153751
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-4 (Compound 1) is a BRD4 inhibitor (IC50=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia .
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- HY-160662
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-5 (example 51) is a BRD4 inhibitor. The Ki values of the two BRD4 domains BDI_K57-E168 and BDII_E352-M457 are 9.7 nM and 16.1 nM, respectively. BRD4-IN-5 can be used in cancer research .
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- HY-142674
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Epigenetic Reader Domain
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Cancer
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BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5) .
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- HY-163413
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- HY-142675
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Epigenetic Reader Domain
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Cancer
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BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) .
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- HY-143299
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- HY-111102
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- HY-153820
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- HY-153459
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation. PROTAC BRD4 Degrader-19 can be used in cancer research .
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- HY-133737
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines .
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- HY-131203
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Epigenetic Reader Domain
Apoptosis
c-Myc
Caspase
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Cancer
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PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .
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- HY-139294
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
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- HY-155393
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- HY-156566
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
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- HY-138632
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively .
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- HY-133136
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- HY-133131
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression .
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- HY-143327
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells .
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- HY-138555
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
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- HY-138637
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
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- HY-143328
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells .
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- HY-136857
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PROTACs
Epigenetic Reader Domain
Ligands for Target Protein for PROTAC
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Cancer
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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 . PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-160527
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Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-25 (Compound 1-f) is a BRD4 degrader. PROTAC BRD4 Degrader-25 can be used for the research of cancer and other bromodomain related diseases .
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- HY-132942
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- HY-132942A
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- HY-138633
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-10 (compound 8b) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 1.3 nM and 18 nM, respectively .
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- HY-138636
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-13 (compound 9d) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-13 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.025 nM and 6.0 nM, respectively .
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- HY-138634
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.23 nM and 0.38 nM, respectively .
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- HY-138635
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively .
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- HY-135558
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- HY-129939
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- HY-129938
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PROTAC-Linker Conjugates for PAC
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Cancer
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PROTAC BRD4 Degrader-24 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker .
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- HY-161093
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PROTACs
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Cancer
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PROTAC BRD4 Degrader-23 (compound 17) is an
effective visible-light-controlled degrader. PROTAC BRD4 Degrader-23 can
inhibit tumor cell proliferation under 405 nm light irradiation .
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- HY-133736
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PROTAC-Linker Conjugates for PAC
ADC Cytotoxin
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Cancer
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PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-144338
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Epigenetic Reader Domain
PARP
Apoptosis
DNA/RNA Synthesis
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Cancer
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PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .
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- HY-107442
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Epigenetic Reader Domain
Ligands for Target Protein for PROTAC
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Cancer
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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) . PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-143471
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Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
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Cancer
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PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity .
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- HY-158031
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Apoptosis
Polo-like Kinase (PLK)
Epigenetic Reader Domain
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Cancer
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PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .
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- HY-150613
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Epigenetic Reader Domain
PARP
Apoptosis
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Cancer
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PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
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- HY-130612
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
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- HY-149948
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
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- HY-156273
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Apoptosis
HDAC
Epigenetic Reader Domain
JAK
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Cancer
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HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo .
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- HY-156828
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Others
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Others
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MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
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- HY-156827
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Others
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Others
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MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
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- HY-161368
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- HY-117997
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Epigenetic Reader Domain
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Cancer
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UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor .
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- HY-161167
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PROTACs
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Cancer
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MM-02-08 is the potent BRD4 degrader and binds to DDB1 .
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- HY-112149A
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Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .
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- HY-157561
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- HY-149098
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Epigenetic Reader Domain
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Cancer
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SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively .
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- HY-107425
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PROTACs
Epigenetic Reader Domain
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Cancer
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MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively .
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- HY-145310
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- HY-151594
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- HY-163019
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- HY-153519
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Epigenetic Reader Domain
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Cancer
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WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
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- HY-151594A
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|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
iBRD4-BD1 diTFA is selective BRD4 bromodomain inhibitor. iBRD4-BD1 diTFA has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 diTFA can be used for the research of inflammation and oncology .
|
-
- HY-149328
-
|
PROTACs
|
Cancer
|
phoBET1 is a photocaged-PROTAC. phoBET1 can achieve BRD4 degradation and effectively suppress tumor growth .
|
-
- HY-112149
-
-
- HY-111977
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4 .
|
-
- HY-111979
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4 .
|
-
- HY-111978
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .
|
-
- HY-129201
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-2759 is a potent BET (Bromodomain and Extra-Terminal Domain) inhibitor, with IC50 values of 0.23, 0.08 and 0.28 μM for BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2), respectively .
|
-
- HY-111139
-
-
- HY-103297
-
-
- HY-153385
-
-
- HY-114902
-
|
Epigenetic Reader Domain
|
Cancer
|
Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
|
-
- HY-125232
-
|
Epigenetic Reader Domain
|
Cancer
|
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .
|
-
- HY-112375
-
|
PROTACs
|
Cancer
|
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4).
|
-
- HY-110378
-
-
- HY-N3213
-
|
Epigenetic Reader Domain
|
Cancer
|
Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) .
|
-
- HY-132991
-
|
PROTAC Linkers
|
Cancer
|
ML 2-14 is a PROTAC for degrading BRD4, with C4 alkyl linker. ML 2-14 exerts degradation of BRD4 in 231MFP breast cancer cells .
|
-
- HY-114305
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation .
|
-
- HY-107425B
-
|
Epigenetic Reader Domain
|
Cancer
|
cis-MZ 1 hydrate is a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The Kd of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively .
|
-
- HY-13235
-
GSK1210151A
|
Epigenetic Reader Domain
|
Cancer
|
I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively .
|
-
- HY-110106
-
GSK1210151A dihydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively .
|
-
- HY-157290
-
|
Epigenetic Reader Domain
Src
|
Cancer
|
HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
|
-
- HY-16954
-
-
- HY-114406
-
|
Ligands for E3 Ligase
|
Cancer
|
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
|
-
- HY-144236
-
|
Epigenetic Reader Domain
|
Others
|
Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis ,and ZLD2218 exhibited the most potent inhibitory activity against BRD4, with the IC50 value of 107 nM
|
-
- HY-44103
-
PROTAC BRD4-binding moiety 4
|
Ligands for Target Protein for PROTAC
|
Cancer
|
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-153945
-
|
Epigenetic Reader Domain
|
Cancer
|
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC50 values of 0.64, 0.25 nM for BRD4-BD1, BRD4-BD2, respectively. BET-IN-15 shows antiproliferative activity .
|
-
- HY-130813
-
-
- HY-102044
-
-
- HY-107443
-
Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
|
Cancer
|
I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1 .
|
-
- HY-112718
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM .
|
-
- HY-130814
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .
|
-
- HY-132941
-
|
PROTACs
|
Cancer
|
CFT-2718 is a new BRD4-targeting degrader (PROTAC) with enhanced catalytic activity and in vivo properties.
|
-
- HY-145264
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
|
-
- HY-136794
-
|
p38 MAPK
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .
|
-
- HY-101460
-
|
|
|
Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC50s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). Tz-Thalidomide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups .
|
-
- HY-147375
-
|
Epigenetic Reader Domain
|
Cancer
|
Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40 .
|
-
- HY-150684
-
|
Epigenetic Reader Domain
|
Cancer
|
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .
|
-
- HY-124859
-
-
- HY-100653A
-
|
Epigenetic Reader Domain
|
Cancer
|
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
|
-
- HY-150683
-
|
Epigenetic Reader Domain
|
Cancer
|
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .
|
-
- HY-131061
-
|
Epigenetic Reader Domain
|
Cancer
|
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 .
|
-
- HY-149878
-
|
Epigenetic Reader Domain
|
Cancer
|
BD-9136 is a highly selective BRD4 degrader. BD-9136 can inhibit tumor growth without adverse effects on mice. BD-9136 can be used for the research of cancer . BD-9136 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-160528
-
|
Epigenetic Reader Domain
Molecular Glues
|
Cancer
|
IBG3 is a dual-JQ1-containing BET degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively .
|
-
- HY-123911
-
-
- HY-124596
-
NKR-P1A
|
Epigenetic Reader Domain
|
Cancer
|
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .
|
-
- HY-153894
-
|
CDK
Epigenetic Reader Domain
PI3K
|
Cancer
|
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells .
|
-
- HY-112398
-
-
- HY-112609
-
-
- HY-111976
-
-
- HY-139620
-
|
PROTACs
|
Cancer
|
MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
|
-
- HY-138563
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
|
-
- HY-157491
-
-
- HY-142520
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .
|
-
- HY-145667
-
Biotin-JQ1
|
Epigenetic Reader Domain
|
Cancer
|
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM .
|
-
- HY-136571
-
GSK046
2 Publications Verification
iBET-BD2
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity .
|
-
- HY-112316B
-
-
- HY-156214
-
AP1867-PEG2-JQ1; AP-PEG2-JQ1
|
Others
|
Others
|
NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins .
|
-
- HY-111916
-
-
- HY-150516S
-
-
- HY-130622
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research .
|
-
- HY-120000
-
MS402
1 Publications Verification
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice .
|
-
- HY-129937A
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
|
-
- HY-16586
-
-
- HY-112376
-
-
- HY-112377
-
-
- HY-112150
-
-
- HY-100670
-
-
- HY-107425A
-
-
- HY-100972
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively .
|
-
- HY-114407
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
|
-
- HY-129937
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .
|
-
- HY-125236
-
|
Epigenetic Reader Domain
|
Cancer
|
BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 inhibits hlL-6 mRNA transcription (IC50 ≤ 0.3 uM), and c-myc activity in human AML MV4-11 cell (IC50 ≤ 0.3 uM)。BET-IN-19 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC50 ≤ 0.3 uM) .
|
-
- HY-100697
-
-
- HY-111502
-
|
Epigenetic Reader Domain
|
Cancer
|
Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM . Antitumor activity .
|
-
- HY-12863
-
CPI-0610
|
Epigenetic Reader Domain
|
Cancer
|
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC .
|
-
- HY-100015
-
ABBV-075
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM .
|
-
- HY-110215
-
|
Epigenetic Reader Domain
|
Cancer
|
XD14 is a potent BET inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with Kds of 170, 380, and 160 nM, respectively .
|
-
- HY-145431
-
|
Epigenetic Reader Domain
Parasite
|
Infection
|
(S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .
|
-
- HY-15846
-
-
- HY-103633
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
|
-
- HY-146741
-
|
Epigenetic Reader Domain
|
Cancer
|
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation .
|
-
- HY-15826
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Inflammation/Immunology
Cancer
|
SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects .
|
-
- HY-114204
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1 .
|
-
- HY-112429
-
HJB97
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
HJB97 is a high-affinity BET inhibitor with Kis of 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. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity .
|
-
- HY-112610
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo .
|
-
- HY-111503
-
|
Epigenetic Reader Domain
|
Cancer
|
Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM .
|
-
- HY-162240
-
-
- HY-111445
-
-
- HY-100696
-
|
|
|
PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1) .
|
-
- HY-13030A
-
|
Epigenetic Reader Domain
|
Cancer
|
(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
|
-
- HY-13959
-
MS436
1 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
|
-
- HY-143317
-
|
Epigenetic Reader Domain
|
Cancer
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-162352
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
SDU-071 is a potent and orally active inhibitor of BRD4-p53 inhibitor. SDU-071 inhibits MDA-MB-231 cells proliferation with an IC50 of 10.5 μM. SDU-071 induces cell cycle arrest and apoptosis .
|
-
- HY-139620A
-
|
PROTACs
|
Others
|
MS83 epimer 1 is the epimer of MS83 (HY-139620). MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder .
|
-
- HY-50698
-
-
- HY-101838
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker .
|
-
- HY-138553A
-
|
Others
|
Cancer
|
(S,R,S)-AHPC-isobutyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is a part of
PROTAC BRD4 Degrader-12 (HY-138635) .
|
-
- HY-153241
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
|
-
- HY-155370
-
|
PROTACs
|
Cancer
|
IR808-TZ?is a potent BRD4 BT-PROTAC?degrader.?IR808-TZ?has the potential for?application in the design of BT-PROTAC targeting other proteins .
|
-
- HY-14443
-
|
ERK
Epigenetic Reader Domain
|
Cancer
|
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity .
|
-
- HY-13960
-
I-BET726
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
|
-
- HY-135236
-
|
Epigenetic Reader Domain
|
Cancer
|
OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity .
|
-
- HY-141844
-
|
HDAC
|
Cancer
|
HDAC/BET-IN-1 displays submicromolar inhibitory activity against HDAC1 and 6 (IC50 = 0.163 μM and 0.067 μM), and BRD4 (Ki = 0.076 μM), and possess potent antileukemia activity.
|
-
- HY-153948
-
|
Epigenetic Reader Domain
|
Cancer
|
CBP-IN-1 (compound 12) is a potent CBP inhibitor, with an IC50 of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4(1), with IC50 values of 690 and 3100 nM, respectively .
|
-
- HY-133139
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-78695
-
|
Epigenetic Reader Domain
PD-1/PD-L1
|
Cancer
|
JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
|
-
- HY-157592
-
|
Epigenetic Reader Domain
|
Cancer
|
MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
|
-
- HY-129917
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
|
-
- HY-131387
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 can be used in PROTAC BRD4 Degrader-5 (HY-133737) and PROTAC BRD4 Degrader-5-CO-PEG3-N3 (HY-133736) .
|
-
- HY-153414
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer .
|
-
- HY-108435
-
-
- HY-133138
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-13030
-
-
- HY-19549
-
|
|
|
RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki values of 3.2-24.7 nM. RX-37 can be used for research of cancers .
|
-
- HY-108369
-
|
PROTAC Linkers
|
Cancer
|
Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 . Azido-PEG1-CH2CO2H is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-122826
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM .
|
-
- HY-147374
-
|
Epigenetic Reader Domain
|
Metabolic Disease
Inflammation/Immunology
|
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .
|
-
- HY-101146
-
SF2523
2 Publications Verification
|
PI3K
Epigenetic Reader Domain
DNA-PK
|
Cancer
|
SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
|
-
- HY-126325
-
|
Epigenetic Reader Domain
|
Cancer
|
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity .
|
-
- HY-157591
-
|
Others
|
Others
|
MMH1-NR, containing a non-reactive (ethyl) group is a negative control of MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
|
-
- HY-132232
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media .
|
-
- HY-123621
-
|
Epigenetic Reader Domain
|
Cancer
|
GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin .
|
-
- HY-146999
-
|
Histone Methyltransferase
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer .
|
-
- HY-15658
-
GSK2801
2 Publications Verification
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .
|
-
- HY-136570A
-
-
- HY-100482
-
-
- HY-100726
-
-
- HY-126428
-
|
HIV
Epigenetic Reader Domain
|
Infection
Inflammation/Immunology
|
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter .
|
-
- HY-163282
-
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
|
-
- HY-101519
-
ZBC 260
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line . BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .
|
-
- HY-120028
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells .
|
-
- HY-149806
-
|
Epigenetic Reader Domain
|
Cancer
|
BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity .
|
-
- HY-136920
-
|
Epigenetic Reader Domain
|
Cancer
|
CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC50=0.01-0.1 µΜ) and BRD4 (IC50=1-1000 µΜ) activity .
|
-
- HY-161125
-
|
Others
|
Others
|
(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .
|
-
- HY-111422
-
|
Epigenetic Reader Domain
|
Cancer
|
PLX51107 is a potent and selective BET inhibitor, with Kds of 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; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
|
-
- HY-112090
-
|
Epigenetic Reader Domain
HIV
|
Infection
Inflammation/Immunology
Cancer
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
|
-
- HY-151593
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .
|
-
- HY-108696
-
GNE-781
2 Publications Verification
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
|
-
- HY-10220
-
|
PI3K
Apoptosis
|
Cancer
|
SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 proagent, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis .
|
-
- HY-136570
-
iBET-BD1
|
Epigenetic Reader Domain
Apoptosis
|
Inflammation/Immunology
Cancer
|
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models .
|
-
- HY-151894
-
|
Epigenetic Reader Domain
|
Cancer
|
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases .
|
-
- HY-134463
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
- HY-114504
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models .
|
-
- HY-111875
-
|
SNIPERs
Epigenetic Reader Domain
|
Cancer
|
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively .
|
-
- HY-149735
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
|
-
- HY-111784
-
CCS1477
|
Epigenetic Reader Domain
|
Cancer
|
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .
|
-
- HY-128341
-
|
ERK
|
Cardiovascular Disease
Cancer
|
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
|
-
- HY-19760
-
|
|
|
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
|
-
- HY-123941
-
dTAG-7
|
PROTACs
FKBP
Epigenetic Reader Domain
|
Cancer
|
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN .
|
-
- HY-19760B
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
|
-
- HY-130984
-
|
PROTAC Linkers
|
Cancer
|
Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-123844
-
dBET57
2 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2 .
|
-
- HY-145226
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies .
|
-
- HY-162077
-
|
HIV
|
Infection
|
HIV-IN-10 is a HIV-1 latency reversing agent .
|
-
- HY-108886
-
JWG-071
1 Publications Verification
|
ERK
|
Cancer
|
JWG-071 is the kinase-selective chemical probe for ERK5. JWG-071 inhibits ERK5 and LRRK2 with IC50 values of 88nM and 109 nM, respectively .
|
-
- HY-148116
-
|
Epigenetic Reader Domain
|
Cancer
|
DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8(1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki>1000 nM) .
|
-
- HY-114421
-
dTAG-13
|
PROTACs
FKBP
|
Cancer
|
FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 F36V and CRBN, thereby selectively degrading FKBP12 F36V .
|
-
- HY-147008
-
|
Epigenetic Reader Domain
|
Cancer
|
XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC) .
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* This product has been "discontinued".
Optimized version of product available:
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Cat. No. |
Product Name |
Chemical Structure |
-
- HY-150516S
-
|
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].
|
-
Cat. No. |
Product Name |
Application |
Reactivity |
-
- HY-P80976
-
BRD4; CAP; HUNK1; MCAP; Bromodomain containing 4; chromosome associated protein
|
WB, IHC-P, ICC/IF, IP
|
Human, Mouse, Rat |
BRD4 Antibody is an antibody about 152 kDa, targeting to BRD4.
|
Cat. No. |
Product Name |
|
Classification |
-
- HY-133736
-
|
|
Azide
|
PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-107442
-
|
|
Alkynes
|
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) . PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-133139
-
|
|
Azide
|
Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-133138
-
|
|
Azide
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Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-108369
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Azide
PROTAC Synthesis
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Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 . Azido-PEG1-CH2CO2H is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-130984
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Azide
PROTAC Synthesis
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Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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