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brd4+protac

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46

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129937A
    GNE-987
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    GNE-987 is a VHL-dependent BRD4 PROTAC degrader. 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 can be used for the research of cancer .
    GNE-987
  • HY-149878

    PROTACs Epigenetic Reader Domain Cancer
    BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity .(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))
    BD-9136
  • 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 .
    TD-106
  • HY-132941

    PROTACs Epigenetic Reader Domain c-Myc Apoptosis Cancer
    CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer .
    CFT-2718
  • HY-107442

    Epigenetic Reader Domain Ligands for Target Protein for PROTAC Cancer
    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.
    PROTAC BRD4-binding moiety 1
  • HY-164995

    PROTACs Epigenetic Reader Domain Drug-Linker Conjugates for ADC Cancer
    L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-171663)) .
    L1BC8
  • HY-174996

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc. (Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)) .
    NEP162
  • HY-161651A

    Epigenetic Reader Domain Cancer
    BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6 (HY-161651). BRD4 ligand 6 TFA is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
    BRD4 ligand 6 TFA
  • 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-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-161651

    Epigenetic Reader Domain Cancer
    BRD4 ligand 6 is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
    BRD4 ligand 6
  • 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-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-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-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-174975

    PROTACs Epigenetic Reader Domain Cancer
    JY-21 is a BRD4 PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells . Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-174994); Black: linker (HY-151862)
    JY-21
  • HY-177730

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))
    PROTAC BRD4 Degrader-40
  • 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-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-153519

    Epigenetic Reader Domain Cancer
    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 .
    WWL0245
  • HY-178510

    PROTACs Epigenetic Reader Domain Cancer
    JQ1-S(GlcNAc)Cq is a sugar-coated BRD4 PROTAC degrader. JQ1-S(GlcNAc)Cq can inhibit the formation of the ternary complex between CRBN and BRD4(BD1/BD2). JQ1-S(GlcNAc)Cq can be used for the research of cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-178514); Black: linker (HY-W105727); BRD4 ligand-Linker: (HY-178519))
    JQ1-S(GlcNAc)Cq
  • 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-176035

    PROTACs Epigenetic Reader Domain Cancer
    MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038) .
    MS479
  • 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-162240

    PROTACs Epigenetic Reader Domain Cancer
    SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research .
    SJH1-51B
  • HY-168692

    PROTAC Linkers Others
    3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol is a linker for BRD4 PROTAC BD-9136 (HY-149878) .
    3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol
  • HY-170383

    E3 Ligase Ligand-Linker Conjugates Others
    CCW16-C4-NHBoc (RNF4 ligand CCW16 (HY-143346)) is an E3 Ligase Ligand-Linker Conjugate for BRD4 PROTAC CCW 28-3 (HY-156774) .
    CCW16-C4-NHBoc
  • HY-157561

    PROTACs Epigenetic Reader Domain Cancer
    K2-B4-3e is a potent BRD4 PROTAC. K2-B4-3e induces BRD4 degradation with a DC50 value of 66 nM .
    K2-B4-3e
  • HY-174997

    E3 Ligase Ligand-Linker Conjugates Cancer
    PFI-7-O-C4-piperazin is a E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs, such as NEP162 (HY-174996). The E3 ligase ligand (PFI-7) of NEP162 is a highly selective antagonist of GID4 (KD = 0.22 μM). NEP162 is a BRD4 PROTAC degrader with anti-tumor activity [1] .
    PFI-7-O-C4-piperazin
  • 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-173433

    Epigenetic Reader Domain Cancer
    JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .
    JV8
  • HY-182801

    PROTACs Epigenetic Reader Domain c-Myc Cancer
    PROTAC BRD4 Degrader-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma .
    PROTAC BRD4 Degrader-46
  • HY-181553

    PROTACs Epigenetic Reader Domain Others
    PROTAC BRD4 Degrader-44 is a BRD4 PROTAC degrader with a DC50 of 16 nM. PROTAC BRD4 Degrader-44 is applicable to studies on membrane-permeable PROTACs .
    PROTAC BRD4 Degrader-44
  • HY-179735

    Ligands for E3 Ligase Cancer
    CRBN ligand-192 is an E3 ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD4 Degrader-41 (HY-179734). PROTAC BRD4 Degrader-41 is a potent BRD4 PROTAC degrader with anti-cancer activity .
    CRBN ligand-192
  • HY-181553A

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells .
    PROTAC BRD4 Degrader-45
  • HY-169401

    E3 Ligase Ligand-Linker Conjugates Others
    L321-NH-C3-PEG3-C1-NH2 (CRBN ligand L321 (HY-169359)) is an E3 Ligase Ligand-Linker Conjugate for BRD4 PROTAC L134 (HY-169358) .
    L321-NH-C3-PEG3-C1-NH2
  • HY-180957

    PROTACs Epigenetic Reader Domain Cancer
    NEP108 is a GID4 E3 ligase-based BRD4 PROTAC degrader, with its DC50 value approximately 3.8 μM. NEP108 has a strong affinity for GID4, with a KD value of 0.22 μM, and the KD value of its trimeric complex is 2.85 μM. NEP108 can be used for cancer research .
    NEP108
  • HY-181495

    Proteasome Cap Targeting Chimeras PROTACs Proteasome Epigenetic Reader Domain Cancer
    RAJQ14 is a BRD4 PROTAC-like CAP-TAC (Proteasome Cap Targeting Chimeras) degrader. RAJQ14 binds to 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14 to recruit target proteins to the proteasome for ubiquitination-independent, proteasome-dependent degradation. RAJQ14 can be used for the research of cancer (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).
    RAJQ14
  • HY-180150

    Epigenetic Reader Domain c-Myc Bcl-2 Family Apoptosis Cancer
    PROTAC BRD4 Degrader-42 (Compound P6) is a PROTAC-based BRD4 degrader with a DC50 of 1.11 μM. PROTAC BRD4 Degrader-42 promotes the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-42 downregulates c-Myc expression and induces Apoptosis by upregulating BAD and BAX protein expression. PROTAC BRD4 Degrader-42 also exhibits anticancer activity against myeloid monocytic leukemia .
    PROTAC BRD4 Degrader-42
  • HY-179734

    PROTACs Epigenetic Reader Domain Apoptosis c-Myc Cancer
    PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc .
    PROTAC BRD4 Degrader-41
  • HY-180889

    PROTACs Epigenetic Reader Domain Neurological Disease Inflammation/Immunology
    PROTAC BRD3 degrader-1 (compound D072) is a potent and selective PROTAC BRD3 degrader. PROTAC BRD3 degrader-1 selectively degrades BRD3 in mice, leading to the downregulation of H3K18ac without affecting BRD2 or BRD4. PROTAC BRD3 degrader-1 reduces intraocular inflammation in the experimental autoimmune uveitis (EAU) mouse mode and inhibits proinflammatory microglia in both uveitis retina and LPS (HY-D1056) treated mouse microglia cell line BV2. PROTAC BRD3 degrader-1 can be used for uveitis research .
    PROTAC BRD3 degrader-1
  • HY-183575

    PROTACs Epigenetic Reader Domain Cancer
    JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia .
    JQ1-JX5
  • HY-107442R

    Reference Standards Epigenetic Reader Domain Ligands for Target Protein for PROTAC Cancer
    PROTAC BRD4-binding moiety 1 (Standard) is the analytical standard of PROTAC BRD4-binding moiety 1 (HY-107442). This product is intended for research and analytical applications. 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.
    PROTAC BRD4-binding moiety 1 (Standard)
  • HY-181868

    E3 Ligase Ligand-Linker Conjugates Cancer
    Lenalidomide-CO-C7-NH2 is a CRBN-dependent intermediate of BET PROTAC degrader. Consisting of the E3 ubiquitin ligase ligand Lenalidomide (HY-A0003) conjugated with a PROTAC linker, Lenalidomide-CO-C7-NH2 induces the protein degradation. By depleting BRD4, PROTAC BET Degrader-16 effectively inhibits cancer cell proliferation, induces cell cycle arrest and promotes apoptosis, thereby exhibiting significant anti-tumor activity in xenograft models. Lenalidomide-CO-C7-NH2 serves as an important tool molecule for the study of acute myeloid leukemia .
    Lenalidomide-CO-C7-NH2
  • HY-181164

    PROTACs Epigenetic Reader Domain HIV Infection
    PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection . (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))
    PROTAC BRD4 Degrader-43

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