Search Result
Results for "
BRD4+inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-50698
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- HY-111139
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- HY-14443
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Epigenetic Reader Domain
ERK
TNK1
CaMK
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Cancer
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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 .
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- HY-107443
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Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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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 .
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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-117491
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-10 (Compound II-25) is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM. BRD4 Inhibitor-10 can be used to study diseases caused by abnormal or excessive cell proliferation, such as cancer .
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- HY-10220
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PI3K
Apoptosis
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Cancer
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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 .
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- HY-112150
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- HY-111916
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- HY-111102
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- HY-112149
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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-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-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-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-132130
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- HY-160499
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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-130813
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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-50698G
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Polo-like Kinase (PLK)
Apoptosis
Epigenetic Reader Domain
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Cancer
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BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription [4].
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- HY-167871
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- HY-172095
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Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-39 (compound 12m) is an orally available BRD4 inhibitor with an IC50 value of 0.02 μM. BRD4 Inhibitor-39 induces apoptosis. BRD4 Inhibitor-39 has anti-tumor activity .
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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-W192171
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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-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-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-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-174812
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- HY-135236
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-160634
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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-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-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-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-W806047
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
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- HY-N16067
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Epigenetic Reader Domain
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Inflammation/Immunology
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Penipanoid C (Compound 9) is a BRD4 inhibitor. Penipanoid C can be isolated from marine sediment-derived fungus Penicillium paneum SD-44. Penipanoid C has anti-inflammatory activity and cytotoxic activity against the SMMC-7721 cells. Penipanoid C can be used for inflammatory diseases research .
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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-132128
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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-170686
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- HY-173062
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Epigenetic Reader Domain
c-Myc
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Others
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BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models .
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- HY-175033
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Epigenetic Reader Domain
Phosphatase
c-Myc
Apoptosis
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Inflammation/Immunology
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BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis .
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- HY-124859
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- HY-160672
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- HY-141843
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- HY-160670
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- HY-160671
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- HY-114902
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Epigenetic Reader Domain
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Cancer
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Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
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- HY-N15522
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Epigenetic Reader Domain
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Cancer
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Bi-magnolignan is a BRD4 inhibitor that induces DNA damage and apoptosis. Bi-magnolignan inhibits HCT116 cell proliferation with an IC50 value of 2.9 μM .
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- HY-162892
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model .
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- HY-104072
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- HY-169994
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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-107443A
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(R)-Molibresib carboxylic acid; (R)-GSK525762A carboxylic acid; (R)-PROTAC BRD4-binding moiety 2
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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(R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1 .
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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-174348
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Epigenetic Reader Domain
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Inflammation/Immunology
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BRD4-IN-10 (Compound 31) is a selective BRD4 inhibitor with an IC50 of 13.5 nM. BRD4-IN-10 can exert anti-inflammatory and anti-fibrotic effects. BRD4-IN-10 also has good metabolic stability, pharmacokinetic properties and safety. BRD4-IN-10 can be used in the research of renal fibrosis diseases .
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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-178984
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PI3K
Epigenetic Reader Domain
DNA/RNA Synthesis
Akt
c-Myc
AMPK
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Cancer
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PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer .
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- HY-125230
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Epigenetic Reader Domain
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Cancer
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CN427 is a quinazoline-based BRD4 inhibitor with a Kd of 66 nM for BRD4. CN427 is applicable to the research of leukemia .
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- HY-180152
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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BRD4 ligand 14 (Compound Y47) is a BRD4 inhibitor. BRD4 ligand 14 exhibits mild anticancer properties against acute myeloid leukemia by inhibiting BRD4. BRD4 ligand 14 can also be used as a ligand for target protein for PROTAC in the development and design of PROTAC BRD4 degraders, such as PROTAC BRD4 Degrader-42 (HY-180150) .
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- HY-107443R
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Molibresib carboxylic acid (Standard); GSK525762A carboxylic acid (Standard); PROTAC BRD4-binding moiety 2 (Standard)
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Reference Standards
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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I-BET762 carboxylic acid (Standard) is the analytical standard of I-BET762 carboxylic acid (HY-107443). This product is intended for research and analytical applications. 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 .
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- HY-107443AR
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(R)-Molibresib carboxylic acid (Standard); (R)-GSK525762A carboxylic acid (Standard); (R)-PROTAC BRD4-binding moiety 2 (Standard)
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Reference Standards
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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(R)-I-BET762 carboxylic acid (Standard) is the analytical standard of (R)-I-BET762 carboxylic acid (HY-107443A). This product is intended for research and analytical applications. (R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1 .
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- HY-181505
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Epigenetic Reader Domain
c-Myc
Bcl-2 Family
PAK
Apoptosis
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Cancer
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BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC) .
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- HY-183922
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PI3K
Epigenetic Reader Domain
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Cancer
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SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC50 values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4BD1, and BRD4BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4BD1 and BRD4BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer[1].
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- HY-115541
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Epigenetic Reader Domain
JAK
FLT3
RET
ROS Kinase
PDGFR
FGFR
c-Myc
STAT
Apoptosis
PARP
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Cancer
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BRD4-IN-41 is a BRD4 inhibitor with an IC50 of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia .
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- HY-182036
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CDK
Epigenetic Reader Domain
Reactive Oxygen Species (ROS)
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Cancer
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KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer .
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- HY-183770
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Akt
PI3K
Epigenetic Reader Domain
c-Myc
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Cancer
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LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma .
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- HY-182671
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PI3K
Btk
Apoptosis
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Cancer
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SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL .
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| Cat. No. |
Product Name |
Type |
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- HY-50698G
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Fluorescent Dyes
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BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription [4].
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| Cat. No. |
Product Name |
Type |
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- HY-50698G
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Biochemical Assay Reagents
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BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription [4].
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-50698G
-
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Polo-like Kinase (PLK)
Apoptosis
Epigenetic Reader Domain
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Cancer
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BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription [4].
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