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E3 ligase Ligand 1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-42424

    VHL Ligand 2 hydrochloride; E3 ligase Ligand 1

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me hydrochloride
  • HY-128808

    E3 ligase Ligand 12

    Ligands for E3 Ligase Cancer
    cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.
    cIAP1 ligand 1
  • HY-128837

    MDM2 Ligand 1; E3 ligase Ligand 16

    Ligands for E3 Ligase Cancer
    Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC .
    Nutlin carboxylic acid
  • HY-42424A

    VHL Ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me dihydrochloride
  • HY-112078

    VHL Ligand 2; E3 ligase Ligand 1A

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
    (S,R,S)-AHPC-Me
  • HY-115446A

    Cereblon Ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride

    E3 Ligase Ligand-Linker Conjugates Cancer
    Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively .
    Lenalidomide-C4-NH2 hydrochloride
  • HY-156499

    Others Others
    RNF114 ligand 1 is a E3 Ubiquitin ligase binder .
    RNF114 ligand 1
  • HY-150799

    Ligands for E3 Ligase Cancer
    CRBN ligand-1 is a ligand for E3 ligase.
    CRBN ligand-1
  • HY-170869

    PROTACs FGFR Cancer
    PROTAC FGFR1 degrader-1 (compound S2H) is a PROTAC degrader targeting FGFR1, with IC50=26.81 nM and DC50=39.78 nM in KG1a cells. PROTAC FGFR1 degrader-1 is composed of CRBN-type E3 ligase ligand (blue part) Pomalidomide (HY-10984), target protein ligand (red part) FGFR1 ligand-1 (HY-170871), and PROTAC linker (black part) 9-Bromononanoic acid (HY-W007587), in which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 164 (HY-170870) .
    PROTAC FGFR1 degrader-1
  • HY-163922

    E3 Ligase Ligand-Linker Conjugates Cancer
    CRBN ligand-1-piperidine-Me is an E3 ligase ligand-linker conjugate.
    CRBN ligand-1-piperidine-Me
  • HY-136772

    E3 Ligase Ligand-Linker Conjugates Others
    Pomalidomide-PEG1-NH2 hydrochloride is a crosslinker-E3 ligase ligand conjugate, consisting of an E3 ligase ligand pomalidomide and a PEGylated crosslinker with terminal amine for reactivity with a carboxyl group on the target ligand .
    Pomalidomide-PEG1-NH2 hydrochloride
  • HY-150885

    Ligands for Target Protein for PROTAC Btk Cancer
    BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies .
    BTK ligand 1
  • HY-170820

    Molecular Glues Cancer
    XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC50=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC50=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
    XYD049
  • HY-168037

    PROTACs PIN1 Cancer
    PROTAC PIN1 degrader-1 (compound D4) is a PROTAC targeting PIN1, with a DC50=1.8 nM. The GI50 of PROTAC PIN1 degrader-1 to MDA-MB-468 is >30 μM. PROTAC PIN1 degrader-1 is composed of target protein ligand PIN1 ligand-1 (HY-168038) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part), and PROTAC linker (black part) [1] .
    PROTAC PIN1 degrader-1
  • HY-W957284

    Ligands for E3 Ligase Cancer
    DCAF11 ligand 1 is the ligand for E3 ligase DCAF11 and can be used for PROTAC synthesis of FF2039 (HY-172159) .
    DCAF11 ligand 1
  • HY-170995

    PROTACs ROR Apoptosis Cancer
    PROTAC ROR1 degrader-1 (Compound 11d) is a PROTAC degrader for pseudokinase ROR1 that degrades ROR1 in NSCLC cells with a DC50s of 40-80 nM. PROTAC ROR1 degrader-1 causes the cleavage of PARP and induces apoptosis in NCI-H23 . (Pink: ligand for target protein ROR1 ligand-1 (HY-170996); Black: linker (HY-W014787); Blue: ligand for VHL E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC ROR1 degrader-1
  • HY-47070

    Ligands for E3 Ligase Others
    VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH 101, acid contains an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand .
    VH 101, acid
  • HY-173066

    PROTACs Indoleamine 2,3-Dioxygenase (IDO) Cancer
    NU227326 is the PROTAC degrader for Indoleamine 2,3-dioxygenase 1 (IDO1) with DC50 of 4.5 nM. NU227326 degrades IDO1 in cell U87 and GBM43 with DC50 of 7.1 nM and 11.8 nM. NU227326 exhibits good pharmacokinetic properties with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours .(Pink: ligand for target protein IDO1 ligand-1 (HY-173067); Black: linker (HY-173068); Blue: ligand for E3 ligase Cereblon (HY-W087383))
    NU227326
  • HY-131886

    E3 Ligase Ligand-Linker Conjugates Cancer
    Pomalidomide 4'-alkylC4-acid (linker16) is a E3 Ligase Ligand-Linker Conjugate. Pomalidomide 4'-alkylC4-acid can be used for conjugation to a target protein ligand .
    Pomalidomide 4'-alkylC4-acid
  • HY-161415

    Ligands for E3 Ligase Cancer
    BCL-xL/BCL-2 ligand 1 (compound 72-1) is a BCL-xL and BCL-2 protein ligand. BCL-xL/BCL-2 ligand 1 can be connected to the E3 ligase by a linker to form PROTACs (HY-161410) .
    BCL-xL/BCL-2 ligand 1
  • HY-159779

    PROTACs Nuclear Hormone Receptor 4A/NR4A Cancer
    NR-V04 is a PROTAC based NR4A1 degrader (Red: NR4A1 inhibitor (HY-13067), black: linker, Blue: E3 ligase ligand) .
    NR-V04
  • HY-163167

    E3 Ligase Ligand-Linker Conjugates Others
    VH 032 amide-alkylC5-amine is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand .
    VH 032 amide-alkylC5-azide
  • HY-163218

    E3 Ligase Ligand-Linker Conjugates Cancer
    PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
    PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid
  • HY-168221

    PROTACs Cancer
    YD54 is a PROTAC based SMARCA2 degrader with a DC50 of 3.5 nM (Red: SMARCA2 degrader (HY-44012B), black: linker, Blue: E3 ligase ligand) .
    YD54
  • HY-163214

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S)-PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
    (S)-PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid
  • HY-131890

    DNA Alkylator/Crosslinker E3 Ligase Ligand-Linker Conjugates Cancer
    VH032 amide-PEG1-acid (linker 10) is a VHL-1 alkyl linker that can be used to bind CDK4/6 ligands (PI) and degradation/destruction tags (EL) (e.g.,E3 ligase ligands) .
    VH032 amide-PEG1-acid
  • HY-141486

    Target Protein Ligand-Linker Conjugates Cancer
    (Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .
    (Rac)-PROTAC PARP/EGFR ligand 1
  • HY-130297

    Bcr-Abl Cancer
    PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1 .
    PROTAC  BCR-ABL1 ligand 1
  • HY-D2336

    PROTACs Cancer
    PROTAC Aster-A degrader-1 (compound NGF3) is a degrader of the sterol transport protein Aster-A. PROTAC Aster-A degrader-1 can be used as a fluorescence probe. (Red: Aster-A inhibitor, black: linker, Blue: E3 ligase ligand) .
    PROTAC Aster-A degrader-1
  • HY-136005

    E3 Ligase Ligand-Linker Conjugates Others
    VH032-C7-COOH is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH032-C7-COOH contains an E3 ligase ligand and an alkyl linker with a terminal amine for conjugation of target protein ligands .
    VH032-C7-COOH
  • HY-161708

    PROTACs CDK FLT3 Cancer
    PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
    PROTAC FLT3/CDKs degrader-1
  • HY-168175

    PROTACs HDAC Cancer
    PROTAC HDAC8 Degrader-2 (compound 32a) is a degrader of HDAC8 with a DC50 of 8.9 nM and HDAC6 with a DC50 of 14.3 nM. PROTAC HDAC8 Degrader-2 is composed of PROTAC target protein ligand HDAC8 ligand 1 (HY-168176) (red part), E3 ligase ligand Thalidomide-4-OH (HY-103596) (blue part) and PROTAC Linker 1,5-Diaminopentane (HY-W540541) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C5-NH2 (HY-134986) .
    PROTAC HDAC8 Degrader-2
  • HY-158551

    PROTACs Bcl-2 Family Cancer
    PROTAC BcI-2/BcI-xI Degrader-1 (15) is a PROTAC based BcI-2/BcI-xI degrader (Red: BcI-2/BcI-xI inhibitor (HY-158677), black: linker, Blue: E3 ligase ligand) .
    PROTAC BcI-2/BcI-xI Degrader-1
  • HY-170872

    PROTACs DNA/RNA Synthesis Cancer
    PT-129 is an RPOTAC degrader targeting the NTF2 domain (protein-RNA interaction site) of G3BP1/2, which mediates the disassembly of intracellular stress granules. PT-129 can inhibit the formation of stress granules in stressed cells and disassemble existing stress granules, and can disrupt the transmission of ATF4, thereby inhibiting the proliferation of cancer cells. Stress granules (SGs) are membrane-less cytoplasmic compartments formed under stress stimuli. SGs promote the transmission of ATF4 from fibroblasts to tumor cells through a migratory effect, mediating fibroblast-related tumor growth. And G3BP1/2 is a central protein of the SGs network, and the inhibition of G3BP1/2 may reduce the stress resistance of cancer cells in the tumor microenvironment. PT-129 is composed of a target protein ligand (red part) G3BP1/2-Targeting ligand-1 (HY-170873), an E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a PROTAC linker (black part) Amino-PEG3-C2-acid (HY-W040165); among them, the E3 ligase ligand + linker form a complex Thalidomide-NH-PEG3-propionic acid (HY-136166) .
    PT-129
  • HY-137340

    PROTACs Cancer
    WH-10417-099 is a CRBN-type PROTAC multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). WH-10417-099 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) PI3Kγ ligand 1 (HY-168319), the E3 ubiquitin ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547) and the PROTAC linker (black part) Amino-PEG5-C2-acid (HY-115384). The E3 ligase ligand and linker can form a conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
    WH-10417-099
  • HY-168863

    PROTACs HDAC Apoptosis Cancer
    FF2049 is a selective HDAC PROTAC degrader (DC50 = 257 nM for HDAC1). FF2049 promotes ubiquitination and degradation of HDAC. FF2049 promotes Apoptosis. FF2049 can be used for the research of hematological and solid cancer (Pink: POI ligand 1 (HY-168864); Blue: E3 ligase FEM1B ligand (HY-168865)) .
    FF2049
  • HY-161958

    PROTACs Histone Acetyltransferase Cancer
    dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961) [1] .
    dCE-2
  • HY-149760

    PROTACs Phosphatase Cancer
    PVD-06 is a selective PROTAC-class PTPN2 degrader (PTPN2/PTP1B selectivity index >60-fold) with anticancer activity. PVD-06 induces PTPN2 degradation via ubiquitination and proteasome-dependent pathways. PVD-06 can promote T cell activation and amplify IFN-γ-mediated cytotoxicity . PVD-06 consists of a target protein ligand (red part) PTPN2 ligand 1 (HY-168691), a PROTAC linker (black part) 6-Aminocaproic acid (HY-B0236), and an E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC-Me (HY-112078). E3 ubiquitin ligase+linker can form 6-Aminocaproic acid-(S,R,S)-AHPC-Me (HY-168690).
    PVD-06
  • HY-168969

    PROTACs Cancer
    AA-BR-157 is a PROTAC degrader for metallothionein 2A (MT2A) with a DC50 of 190 nM. AA-BR-157 downregulates the cytoskeleton and cell motility regulating protein DIAPH3, inhibits the migration of MDA-MB-231 and U-87 MG. AA-BR-157 regulates the zinc homeostasis in MDA-MB-231 . (Pink: ligand for target protein MT2A ligand 1 (HY-168970); Black: linker (HY-119429); Blue: ligand for VHL E3 ligase (HY-125845))
    AA-BR-157
  • HY-168190

    PROTACs Cancer
    PROTAC TBL1X degrader-1 (Compound TD11) is a PROTAC degrader for Transducin β-like protein 1 X-linked (TBL1X), and exhibits cytotoxicity in lymphoma cell Riva, Pfeiffer and Granta-519 with IC50 of 0.795, 0.397 and 0.522 μM, respectively. (Pink: ligand for target protein: TBL1X ligand 1 (HY-168191); Black: linker (HY-168193); Blue: ligand for E3 ligase: Thalidomide 4-fluoride (HY-41547))
    PROTAC TBL1X degrader-1
  • HY-134850

    PROTACs Tau Protein Neurological Disease
    QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau. QC-01-175 reduces the levels of A152T and P301L mutant tau protein and protects neurons from tau-mediated toxicity and improve cell survival (Pink: ligand for target protein Aberrant tau ligand 1 (HY-W453397); Black: linker NH2-PEG3 (HY-W007545); Blue: ligand for E3 ligase Pomalidomide (HY-10984)) .
    QC-01–175
  • HY-173082

    PROTACs FKBP Cancer
    10-SLF is a PROTAC FKBP12 degrader. 10-SLF induces a ternary complex between FKBP12 and FBXW7-R465C, and promotes FBXW7-R465C-dependent proteasomal degradation of FKBP12. 10-SLF selectively reduces FKBP12 levels in cells expressing FBXW7-R465C. Pink: FKBP12 ligand (HY-170988); Black: linker (HY-W004640); Blue: E3 ligase ligand .
    10-SLF
  • HY-162816

    PROTACs MAP4K Cancer
    PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841) [1] .
    PROTAC HPK1 Degrader-3
  • HY-172368

    PROTACs Histone Methyltransferase IKZF Family Apoptosis Inflammation/Immunology Cancer
    PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research . (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
    PROTAC CARM1/IKZF3 degrader-1

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