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BRD4 Degrader

" in MedChemExpress (MCE) Product Catalog:

155

Inhibitors & Agonists

8

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163638

    Molecular Glues Epigenetic Reader Domain E1/E2/E3 Enzyme Cancer
    BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue BRD4 degrader. BRD4 degrader-1 targets DCAF16 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
    BRD4 degrader-1
  • HY-136857

    Epigenetic Reader Domain Cancer
    BRD4 degrader-3 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.
    BRD4 degrader-3
  • HY-111433
    BRD4 degrader AT1
    2 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    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.
    BRD4 degrader AT1
  • HY-138632

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-9
  • HY-160527

    Epigenetic Reader Domain Cancer
    BRD4 degrader-4 (Compound 1-f) is a BRD4 degrader. BRD4 degrader-4 can be used for the research of cancer and other bromodomain related diseases .
    BRD4 degrader-4
  • HY-163639

    Molecular Glues Epigenetic Reader Domain E1/E2/E3 Enzyme Cancer
    BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
    BRD4 degrader-2
  • HY-170989

    AUTACs Epigenetic Reader Domain Autophagy Cancer
    BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM .
    BRD4 degrader-5
  • HY-173327

    PROTACs Epigenetic Reader Domain Cancer
    BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity .
    BRD4 degrader-6
  • HY-174210

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics . Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)
    PROTAC BRD4 Degrader-31
  • HY-175240

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28 .Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)
    PROTAC BRD4 Degrader-38
  • HY-133136

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1 .
    PROTAC BRD4 Degrader-2
  • HY-174811

    PROTACs Epigenetic Reader Domain PD-1/PD-L1 Inflammation/Immunology Cancer
    PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC BRD4 Degrader-33
  • HY-133737

    PROTAC BRD4 Degrader-5

    PROTACs Epigenetic Reader Domain Cancer
    GAL-02-221 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GAL-02-221 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines .
    GAL-02-221
  • HY-133131

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-1
  • HY-143327

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    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 .
    PROTAC BRD4 Degrader-16
  • HY-177041

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase) .
    PROTAC BRD4 Degrader-35
  • HY-143328

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    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 .
    PROTAC BRD4 Degrader-17
  • HY-139294

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-15
  • HY-138555

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-8
  • HY-138637

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-14
  • HY-176449

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-32 (Compound 22) is a BRD4 PROTAC degrader (DC50: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies). (Pink: GSK1324726A (HY-13960); Black: linker (HY-176450); Blue: Lenalidomide-5-Br (HY-W072954)) .
    PROTAC BRD4 Degrader-32
  • HY-175767

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))
    PROTAC BRD4 Degrader-39
  • HY-153820

    Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD4 Degrader-20 (compound 195) is an bifunctional compound and an degrader of BRD4 .
    PROTAC BRD4 Degrader-20
  • HY-175224

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-36 has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. PROTAC BRD4 Degrader-36 is cytotoxic to PANC-1 cells (GI50: 0.103 μM). PROTAC BRD4 Degrader-36 can be used in the study of cancer. (Pink: PROTAC BRD4 ligand-1 (HY-129939); Blue + Black: E3 ligase ligand + linker (HY-175241)) .
    PROTAC BRD4 Degrader-36
  • HY-174920

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective BRD4 PROTAC degrader (pDC50 = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)) .
    PROTAC BRD4 Degrader-34
  • HY-156566

    Epigenetic Reader Domain PROTACs Cancer
    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 .
    PROTAC BRD4 Degrader-21
  • HY-138635

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-12
  • HY-138633

    PROTACs Epigenetic Reader Domain Cancer
    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 .
    PROTAC BRD4 Degrader-10
  • HY-133736

    PROTAC-Linker Conjugates for PAC ADC Payload Cancer
    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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
  • HY-175225

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-37 (Compound TrimTAC-2) is a PROTAC BRD4 degrader. PROTAC BRD4 Degrader-37 has a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI50: 0.282 μM). PROTAC BRD4 Degrader-37 can be used in the research of tumors. (Pink: PROTAC BRD4 ligand-4 (HY-175242); Blue + Black: E3 ligase ligand + linker (HY-175241)) .
    PROTAC BRD4 Degrader-37
  • HY-131203

    PROTACs Epigenetic Reader Domain Apoptosis c-Myc Caspase Cancer
    PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC 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 (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)) .
    PROTAC BRD4 Degrader-6
  • HY-135558

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4 .
    PROTAC BRD4 Degrader-3
  • HY-155393

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC50 (MOLT4, 24 h) of 9.2 .
    PROTAC BRD4 Degrader-22
  • HY-161650

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC, which degrades 80% BRD4 at 1 μM by using photocleavable linker. PROTAC BRD4 Degrader-26 will be deactivated by UV light. (Pink: ligand for target protein BRD4 ligand 6 (HY-161651); Black: linker (HY-161653); Blue: E3 ligase ligand Thalidomide 4-fluoride (HY-41547))
    PROTAC BRD4 Degrader-26
  • HY-161093

    PROTACs Cancer
    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 .
    PROTAC BRD4 Degrader-23
  • HY-172124

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-29 (compound 7a) is a potent PROTACs degrader of BRD4, with the DC50 of 89.4 nM. PROTAC BRD4 Degrader-29 plays an important role in cancer research (Pink: ligand for target protein (HY-13030); Black: linker (HY-172125); Blue: E3 ligase ligand (HY-103597)) .
    PROTAC BRD4 Degrader-29
  • HY-170808

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)) .
    PROTAC BRD4 Degrader-28
  • HY-162875

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC BRD4 Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC BRD4 ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875) [1] .
    PROTAC BRD4 Degrader-27
  • HY-169151

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)) .
    PROTAC BRD4-DCAF1 degrader-1
  • HY-160694

    cBu-Cit-PROTAC BRD4 Degrader-5

    PROTAC-Linker Conjugates for PAC Epigenetic Reader Domain Cancer
    cBu-Cit-GAL-02-221 is a PROTAC that degrades BRD4 by association with cBu-Cit. cBu-Cit-GAL-02-221 can effectively inhibit BRD4 in HER2 positive and negative breast cancer cell lines. cBu-Cit-GAL-02-221 has a single bond and can be conjugated to an ADC antibody to form a PAC .
    cBu-Cit-GAL-02-221
  • HY-176477

    Epigenetic Reader Domain FKBP Cancer
    BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212) .
    BRD4/FKBP12 degrader-2
  • HY-176476

    Epigenetic Reader Domain FKBP Cancer
    BRD4/FKBP12 degrader-1(a1d) is a BRD4/FKBP12 degrader with anti-cancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176501, linker: HY-140212) .
    BRD4/FKBP12 degrader-1
  • HY-130612

    Epigenetic Reader Domain PROTACs Cancer
    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 .
    PROTAC BRD2/BRD4 degrader-1
  • HY-149948

    Epigenetic Reader Domain PROTACs Cancer
    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 .
    PROTAC BRD3/BRD4-L degrader-2
  • HY-175610

    PROTACs FLT3 JAK Epigenetic Reader Domain Cancer
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
    PROTAC FLT3/JAK2/BRD4 Degrader-1
  • HY-156827

    Molecular Glues Epigenetic Reader Domain Cancer
    MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
    MMH1
  • HY-156828

    Molecular Glues Epigenetic Reader Domain Cancer
    MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
    MMH2
  • HY-161368

    PROTACs Epigenetic Reader Domain Cancer
    BRD-SF2 is a BRD4-targeted PROTAC degrader (DC50: 17.2 μM) (Blue: VHL ligand, black: linker, pink: BRD4 ligand) .
    BRD-SF2
  • HY-176071

    ByeTAC Epigenetic Reader Domain Cancer
    TEC 4 is a ByeTAC (Bypassing E-Ligase-Targeting Chimera) BRD4 degrader, with 33% BRD4 remaining at 500 nM in Ramos B-cells. TEC 4 shows toxicity for Ramos B-cells, with an IC50 of 30.5 nM. ByeTACs directly recruits a protein to the proteasome via interactions with Rpn-13 for degradation. Pink: BRD4 lignad (HY-78695); Blue: Rpn-13 ligand (HY-159808); Black: linker (HY-W008352) .
    TEC 4
  • HY-163019

    Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain Metabolic Disease
    EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs) .
    EN884

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