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Photocagedproteolysis-targeting chimera (PROTAC)

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5366

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6

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6

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19

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13

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7

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20

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9

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974

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6

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-152227

    PROTACs JAK Inflammation/Immunology
    PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1 has TYK2 degradation activity with DC50 value of 14 nM. PROTAC TYK2 degradation agent1 can be used for the research of autoimmune disease .
    PROTAC TYK2 degradation agent1
  • HY-111758
    PROTAC B-Raf degrader 1
    1 Publications Verification

    PROTACs Raf Cancer
    PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity .
    PROTAC B-Raf degrader 1
  • HY-125877
    PROTAC Mcl1 degrader-1
    1 Publications Verification

    PROTACs Bcl-2 Family Cancer
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .
    PROTAC Mcl1 degrader-1
  • HY-141486A

    PARP EGFR Ligands for Target Protein for PROTAC Others
    PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology .
    PROTAC PARP/EGFR ligand 1
  • 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-148381

    Epigenetic Reader Domain PROTACs Apoptosis Cancer
    A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer .
    A947
  • HY-174877

    PROTACs HDAC Cancer
    PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ∼50% Dmax only upon activation to its cis-state with 390 nm light irradiation . Pink: HDAC6 ligand; Blue: CRBN ligase ligand (HY-A0003); Black: linker
    PROTAC HDAC6 degrader 6
  • HY-155371

    PROTACs Others
    BT-PROTAC is a bioorthogonally activatable prodrug. BT-PROTAC can accurately control the activity of PROTAC .
    BT-PROTAC
  • HY-P10446

    Epigenetic Reader Domain PROTACs Cancer
    TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .
    TAT-PiET-PROTAC
  • HY-162106

    Ferroptosis PROTACs Glutathione Peroxidase Cancer
    PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
    PROTAC GPX4 degrader-2
  • HY-146423

    PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .
    PROTAC EGFR degrader 6
  • HY-146422

    PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .
    PROTAC EGFR degrader 5
  • HY-149434

    Androgen Receptor PROTACs Apoptosis Cancer
    PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
    PROTAC AR-NTD degrader 1
  • HY-155361

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC50 = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies. (Pink: BI 7271: HY-123616, Blue: 5-Aminothalidomide: HY-W023573, Blue + Black: Thalidomide-5-piperazine: HY-W834174, Black: N,N'-Dimethylpiperazine: HY-W539783) .
    PROTAC BRD9 Degrader-7
  • HY-173135

    PROTACs Histone Demethylase Apoptosis Cancer
    PROTAC KDM4 degrader-1 (Compound 11) is a KDM4-targeted proteolysis targeting chimeras (PROTAC) degrader. PROTAC KDM4 degrader-1 can degrade KDM4A-C while sparing KDM4D. PROTAC KDM4 degrader-1 exhibits potent antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 induces apoptosis and cell cycle arrest, and inhibits histone H3 lysine demethylation. (Blue: E3 ligase ligand (HY-112078), Black: linker (HY-W013381); Pink: ligand for target protein (HY-173136) ) .
    PROTAC KDM4 degrader-1
  • HY-163445

    NAMPT Cancer
    NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .
    NAMPT activator-6
  • HY-143344

    PROTACs CFTR Inflammation/Immunology
    NJH-2-056 is a deubiquitinase-targeting chimera (DUBTAC) linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor. NJH-2-056 can be used for cystic fibrosis research .
    NJH-2-056
  • HY-146393
    PROTAC CYP1B1 degrader-1
    1 Publications Verification

    PROTACs Cytochrome P450 Cancer
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
    PROTAC CYP1B1 degrader-1
  • HY-168456

    Ligands for Target Protein for PROTAC Infection
    RNA recruiter 1 is the RNA ligand of RNAse L RIBOTAC (HY-168456), an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNA recruiter 1 can be utilized in the synthesis of RIBOTAC .
    RNA recruiter 1
  • HY-122829

    PROTACs BCL6 Cancer
    BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research .
    BCL6 PROTAC 1
  • HY-135312

    Estrogen Receptor/ERR PROTACs Cancer
    AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer .
    AZ'6421
  • HY-143343

    Wee1 Cancer
    LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker .
    LEB-03-153
  • HY-162241

    PROTACs Others
    SJH1-62B is a proteolysis targeting chimera (PROTAC) that can target the androgen receptor (AR) .
    SJH1-62B
  • HY-168457

    SARS-CoV Others
    RNase L ligand 2 (compound 6) is the Rnase L ligand part of RNAse L RIBOTAC (HY-168455), an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNase L ligand 2 can be used in the synthesis of RIBOTAC .
    RNase L ligand 2
  • HY-147373

    PROTACs Ligands for E3 Ligase Cancer
    DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research .
    DA-PROTAC
  • HY-143340

    Wee1 Cancer
    LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker .
    LEB-03-145
  • HY-147174

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker .
    PROTAC_ERRα
  • HY-122828

    PROTACs Btk Others
    PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels .
    PROTAC BTK Degrader-2
  • HY-125878
    PROTAC SGK3 degrader-1
    4 Publications Verification

    SGK3-PROTAC1

    PROTACs SGK Cancer
    PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate) .
    PROTAC SGK3 degrader-1
  • HY-168458

    Target Protein Ligand-Linker Conjugates Infection
    RNA recruiter-linker 1 is the RNA ligand-linker part of RNAse L RIBOTAC (HY-168455), an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNA recruiter-linker 1 can be utilized in the synthesis of RIBOTAC .
    RNA recruiter-linker 1
  • HY-173009

    PROTACs Cyclophilin HCV HIV Infection
    PROTAC CG167 is a selective and potent CypA PROTAC degrader. PROTAC CG167 degrades CypA in a dose-dependent manner (Jurkat: DC50: 123 nM). PROTAC CG167 can inhibit HIV-1 and HCV and exhibits antiviral activity . (Pink: CypA Ligand (HY-170997); Black: Linker (HY-W123015); Blue: E3 Ligase Ligand (HY-112078))
    PROTAC CG167
  • HY-161108

    PROTACs Checkpoint Kinase (Chk) Cancer
    PROTAC Chk1 degrader-1 (Compound PROTAC-2 ) is a potent PROTAC-targeted degrader of Chk1 with a DC50 of 1.33 μM. PROTAC Chk1 degrader-1 can be used in cancer research .
    PROTAC Chk1 degrader-1
  • HY-162876

    Ligands for Target Protein for PROTAC Cancer
    PROTAC BRD4 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PROTAC BRD4 ligand-3 can be used for synthesis PROTAC BRD4 Degrader-27 (HY-162875) .
    PROTAC BRD4 ligand-3
  • HY-114229
    PROTAC BET degrader-3
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET Degrader-3 is a PROTAC connected by ligands for von Hippel-Lindau and BET.
    PROTAC BET degrader-3
  • HY-145073

    PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
    PROTAC ER Degrader-10
  • HY-135345
    PROTAC FKBP Degrader-3
    1 Publications Verification

    PROTACs FKBP Cancer
    PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
    PROTAC FKBP Degrader-3
  • HY-143458

    FAK PROTACs Cancer
    FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion .
    FAK PROTAC B5
  • HY-161749

    PROTACs Anaplastic lymphoma kinase (ALK) Cancer
    PROTAC ALK degrader-1 (compound B1) is an ALK degrader based on PROTACs, with the DC50 of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability .
    PROTAC ALK degrader-1
  • HY-112100

    PROTAC-Linker Conjugates for PAC Estrogen Receptor/ERR Cancer
    PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
    PROTAC ERα Degrader-5
  • HY-156591

    PROTACs Mixed Lineage Kinase Others
    PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax >90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
    PROTAC MLKL Degrader-1
  • HY-169072

    PROTACs Mixed Lineage Kinase Cancer
    PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074) [1] .
    PROTAC MLKL Degrader-2
  • HY-148334

    PROTACs Histone Methyltransferase Cancer
    MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC) .
    MS8815
  • HY-155356A

    PROTACs Cancer
    YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356). YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth .
    YN14 (mixture of diastereomers)
  • HY-168311

    Ligands for Target Protein for PROTAC Cancer
    PROTAC IRAK4 ligand-5 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PROTAC IRAK4 ligand-5 can be utilized for the synthesis of KT-413 (HY-153368) .
    PROTAC IRAK4 ligand-5
  • HY-168611

    Ligands for Target Protein for PROTAC IRAK Cancer
    PROTAC IRAK4 ligand-4 is a Ligand for Target Protein for PROTAC with antitumor activity. PROTAC IRAK4 ligand-4 can be used to synthesize PROTAC IRAK4 degrader-12 (HY-168586) .
    PROTAC IRAK4 ligand-4
  • HY-149678

    PROTACs Cancer
    PROTAC eDHFR Degrader-1 is a PROTAC that is effective degradation of eDHFR-YFP, various POIs-including YFP and Luciferase .
    PROTAC eDHFR Degrader-1
  • HY-153415

    PROTACs Bcr-Abl Cancer
    PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer .
    PROTAC BCR-ABL Degrader-1
  • HY-123961

    PROTACs c-Met/HGFR Cancer
    SJF-8240 (PROTAC 7) is a proteolysis targeting chimera (PROTAC) degrader. SJF-8240 induces polyubiquitination of c-Met and inhibits the proliferation of GTL16 cells (IC50=66.7 nM) .
    SJF-8240
  • HY-158152

    Ligands for E3 Ligase Cancer
    PROTAC CRBN ligand-2 (12) is a Biguanide-PROTAC derivative, with an EC50 of 0.15 mM in KP4 cells. PROTAC CRBN ligand-2 (12) demonstrates the ability to alter levels of mitochondrial proteins, notably complexes I and IV .
    PROTAC CRBN ligand-2
  • HY-157763

    PROTAC-Linker Conjugates for PAC Btk Cancer
    PROTAC BTK Degrader-8 (compound 3) is an effective PROTAC BTK degrader that can be coupled to an ADC antibody to form a PAC.
    PROTAC BTK Degrader-8

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