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E3+Ligand

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41

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3

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-176786
    MCB-36

    		PROTACs Ras Apoptosis PERK p38 MAPK Caspase TNF Receptor Cancer
    MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
    MCB-36
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    		PROTACs PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
    PROTAC PD-1/PD-L1 degrader-1
  • HY-129523
    PROTAC K-Ras Degrader-1
    2 Publications Verification

    		 PROTACs Ras Cancer
    PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells .
    PROTAC K-Ras Degrader-1
  • HY-130122
    MG-277
    1 Publications Verification

    		 Molecular Glues PROTACs Apoptosis Cancer
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
    MG-277
  • HY-114324
    PROTAC PARP1 degrader

    		PROTACs PARP Cancer
    PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader consists of E3 ubiquitinase ligand MDM2 ligand (HY-128836), blue part; target protein ligand PAPR1 ligand (HY-171543), pink part; PROTAC linker N3-PEG4-C2-NH2 (HY-128834), black part .
    PROTAC PARP1 degrader
  • HY-W410002
    Pomalidomide-propargyl

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Pomalidomide-propargyl contains an E3 ligand and a terminal alkyl group ready for click conjugation. Pomalidomide-propargyl is ready for conjugation to target proteins for PROTAC.
    Pomalidomide-propargyl
  • HY-115881
    SR-1114

    		PROTACs Epigenetic Reader Domain Cancer
    SR-1114 is a PROTAC degrader targeting ENL. SR-1114 degrades ENL in a CRBN-dependent manner and selectively downregulates ENL target genes. SR-1114 can promote the differentiation of acute myeloid leukemia cells. SR-1114 can be used in tumor research. (Pink: ENL ligand (HY-145409); Black: Linker; Blue: E3 Ligand (HY-14658)) .
    SR-1114
  • HY-171768
    SK2187

    JB301

    		 PROTACs Aurora Kinase Neurological Disease Cancer
    SK2187 is a selective AURKA PROTAC degrader with a DC50 of about 10 nM. SK2187 exhibits growth inhibition against NGP cells with an IC50 of 101.5 nM. SK2187 can be used for the study of MYCN-amplified neuroblastoma (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: E3 ligand (HY-103597); Black: Linker: Amino-PEG3-alcohol (HY-W015088)) .
    SK2187
  • HY-162702
    AZ'3137

    		PROTACs Androgen Receptor Cancer
    AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Pink: AR Ligand (HY-172954); Blue: CRBN ligand (HY-172955); Black: linker (HY-W262798); E3 Ligand+Linker: HY-172956) .
    AZ'3137
  • HY-164864
    DU-14 (PTP1B/TC-PTP PROTAC)

    		PROTACs STAT Cancer
    DU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity. (Pink: PTP1B/TC-PTP inhibitor (HY-171027); Black: Linker (HY-W340290); Blue: E3 ligand (HY-112078)) .
    DU-14 (PTP1B/TC-PTP PROTAC)
  • HY-175252
    PROTAC EGFR degrader 14

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFR C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)) .
    PROTAC EGFR degrader 14
  • HY-157566
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride

    		Ligands for E3 Ligase Cancer
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated .
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride
  • HY-171769
    dAurAB2

    		PROTACs Aurora Kinase Cancer
    dAurAB2 is a dual-degrading PROTAC that potently degrades Aurora-A and Aurora-B with DC50s of 59 nM and 39 nM, respectively. dAurAB2 reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells. dAurAB2 can be used for the study of neuroblastoma. (Pink, Aurora ligand (HY-10804); Blue, E3 ligand: (HY-103597); Black, linker (HY-W105740)) .
    dAurAB2
  • HY-175766
    CRBN Ligand-Linker Conjugate 2

    		E3 Ligase Ligand-Linker Conjugates Inflammation/Immunology
    CRBN Ligand-Linker Conjugate 2 is a synthesized E3 ligand-linker conjugate that can be used for synthesis of PROTACs, such as FIP22 (HY-175764). FIP22 is a potent and selective IRAK4 PROTAC degrader with anti- atopic dermatitis activity .
    CRBN Ligand-Linker Conjugate 2
  • HY-114324A
    rel-PROTAC PARP1 degrader

    		PROTACs PARP Cancer
    rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
    rel-PROTAC PARP1 degrader
  • HY-175525
    MS44

    		PROTACs Aurora Kinase Cancer
    MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand (HY-175526); Blue: E3 ligand (HY-112078); Black: Linker; E3 ligand + Linker (HY-132938)) .
    MS44
  • HY-147192
    (S,R,S)-AHPC-O-PEG1-propargyl

    		E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-O-PEG1-propargyl (Compound 10b) is an E3 ligand for the synthesis of PROTAC . (S,R,S)-AHPC-O-PEG1-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (S,R,S)-AHPC-O-PEG1-propargyl
  • HY-174867
    AY-4

    		PROTACs Ferroptosis Cancer
    AY-4 (Compound AY-4) is an efficient PROTAC degrader targeting FTH1 (Kd = 3.17 nM). AY-4 effectively upregulates the levels of ferrous (Fe 2+) and ferric (Fe 3+) ions in cells. AY-4 is a potential anticancer candidate compound that regulates iron homeostasis through ferritin degradation and enhances the efficacy of existing drugs. AY-4 can effectively reduce the level of FTH1 in breast cancer cells (Pink: FTH1 ligand AY-2 (HY-174871); Blue: E3 ligand Pomalidomide (HY-10984); Black: Linker, Pomalidomide-PEG3-acid (HY-174872)) .
    AY-4
  • HY-175321
    PROTAC c-Met degrader-6

    		PROTACs c-Met/HGFR Apoptosis Cancer
    PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer (Pink: c-Met ligand (HY-W425461); Blue: E3 ligand (HY-14658); Black: Linker (HY-20797)) .
    PROTAC c-Met degrader-6
  • HY-W998278A
    Desamino lenalidomide-acetylene-C2-NH2 TFA

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Desamino lenalidomide-acetylene-C2-NH2 TFA is an E3 ligand-linker conjugate that incorporates a ligand based on CRBN and a linker, and can be used for the synthesis of PROTAC.
    Desamino lenalidomide-acetylene-C2-NH2 TFA
  • HY-161132
    Lenalidomide 4'-alkyl-C5-azide

    		E3 Ligase Ligand-Linker Conjugates Others
    Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand for PROTAC development that contains an E3 ligand and an alkyl LC5 ligand with terminal azides that can be coupled to a target protein ligand .
    Lenalidomide 4'-alkyl-C5-azide
  • HY-179305
    CBM-4077

    		Ligands for E3 Ligase Cancer
    CBM-4077 is a PROTAC E3 ligand that can be used for synthesis of PROTACs, such as BCL6-760 (HY-178777). BCL6-760 is a potent BCL6 PROTAC degrader with anti-tumor activity .
    CBM-4077
  • HY-158313
    PROTAC EGFR degrader 13

    		EGFR PROTACs Cancer
    PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-14658); Black: linker (HY-W262798); E3 ligand + linker: HY-W998306) .
    PROTAC EGFR degrader 13
  • HY-163845
    YX862

    		PROTACs HDAC Cancer
    YX862 is a selective HDAC8 PROTAC degrader and induces the degradation of HDAC8 with maximum degradation ＞ 95% at 250 nM in MDA-MB-231 cells(Sturcture Note:(Blue: VHL E3 ligand (HY-112078), Black: linker；Pink: HDAC8 inhibitor (HY-163846)) .
    YX862
  • HY-175867
    PROTAC SMARCA2 degrader-34

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2 degrader-34 (compound 52) is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: < 0.1 μM for SMARCA2, > 1 μM for SMARCA4). PROTAC SMARCA2 degrader-34 can be used for study of cancer. (Pink: SMARCA2 ligand (HY-178414) ; Blue: E3 ligand (HY-168055) ; Black: linker) .
    PROTAC SMARCA2 degrader-34
  • HY-155072
    PROTAC BTK Degrader-5

    		PROTACs Btk Cancer
    PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297；Pink:BKT inhibitor (HY-150898)) 1.
    PROTAC BTK Degrader-5
  • HY-174858
    dASK1-VHL

    		PROTACs ASK1 p38 MAPK Metabolic Disease
    dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH) (Pink: ASK1 ligand 1 (HY-174860); Blue: E3 ligand (S,R,S)-AHPC (HY-125845); Black: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861) .
    dASK1-VHL
  • HY-148834
    Pomalidomide-piperazine

    		Ligands for E3 Ligase Others
    Pomalidomide-piperazine is an active compound that can be used to synthesis the E3 ligand for PROTAC .
    Pomalidomide-piperazine
  • HY-168225
    PROTAC SMARCA2/4-degrader-35

    		PROTACs Others
    PROTAC SMARCA2/4-degrader-35 (Ex.43) is a SMARCA2/4 degrader with a DC50 <2.5 nM. (Target ligand: HY-W874018; E3 ligand: HY-168226; linker: HY-168227; E3 ligand+linker: HY-168228)
    PROTAC SMARCA2/4-degrader-35
  • HY-169010
    Pomalidomide-CO-C5-Br

    		E3 Ligase Ligand-Linker Conjugates Infection
    Pomalidomide-CO-C5-Br (Compound 6b) is a conjugated compound of the E3 ligand Pomalidomide and linker. It can be used to synthesize highly effective PROTAC molecules targeting ADC (HY-169008) .
    Pomalidomide-CO-C5-Br
  • HY-163209
    VH 032 amide-PEG6-amine hydrochloride

    (S,R,S)-AHPC-PEG6-NH2 hydrochloride

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    VH 032 amide-PEG6-amine hydrochloride (Step 4) is a functionalized von-Hippel-Lindau protein-ligand (VHL) for PROTAC development, consisting of an E3 ligand and a PEG6 ligand. Terminal amines can be coupled to target protein ligands .
    VH 032 amide-PEG6-amine hydrochloride
  • HY-175547
    PROTAC HPK1 Degrader-5

    		PROTACs MAP4K ERK Interleukin Related IFNAR Inflammation/Immunology Cancer
    PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)) .
    PROTAC HPK1 Degrader-5
  • HY-169008
    PROTAC ACC degrader-1

    		PROTACs Acetyl-CoA Carboxylase Infection
    PROTAC ACC degrader-1 (Compound 9b) is a Acetyl-CoA Carboxylase degrader. PROTAC ACC degrader-1 exhibits superior potency against Aphis craccivora (IC50 = 107.8 μg/mL). (Structure Note: Pink, Target protein ligand (HY-169009); Blue, E3 ligand (HY-10984); Black, linker (HY-W007559) .
    PROTAC ACC degrader-1
  • HY-179733
    CRBN ligand-191

    		Ligands for E3 Ligase Cancer
    CRBN ligand-191 is an E3 ligand that can be used for the synthesis of PROTACs, such as PROTAC ALK degrader-4 (HY-179732) .
    CRBN ligand-191
  • HY-180986
    cis-Lenalidomide-CO-Ph-N2-Ph-O-C4-Cl

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Cis-Lenalidomide-CO-Ph-N2-Ph-O-C4-Cl is a synthetic E3 ligand-connector conjugate that can be used for the synthesis of Azo-PROTAC-4C-cis (HY-180985).
    cis-Lenalidomide-CO-Ph-N2-Ph-O-C4-Cl
  • HY-179735
    CRBN ligand-192

    		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-168228
    E3 Ligase Ligand-linker Conjugate 123

    		E3 Ligase Ligand-Linker Conjugates Others
    E3 Ligase Ligand-linker Conjugate 123 is the E3 ligand-linker part of PROTAC SMARCA2/4-degrader-35 (HY-168225). E3 Ligase Ligand-linker Conjugate 123 can be utilized in the synthesis of PROTACs .
    E3 Ligase Ligand-linker Conjugate 123
  • HY-180961
    His-TERRα

    		PROTACs Estrogen Receptor/ERR Cancer
    His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer .
    His-TERRα
  • HY-175445
    GNE-5472

    		PROTACs Estrogen Receptor/ERR IAP NF-κB TNF Receptor Apoptosis Cancer
    GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .
    GNE-5472
  • HY-180925
    Leu-PEG1-Dasa

    		PROTACs Bcr-Abl Cancer
    Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML) .
    Leu-PEG1-Dasa
  • HY-180962
    Phe-PEG1-Dasa

    		PROTACs Bcr-Abl Cancer
    Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia .
    Phe-PEG1-Dasa

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