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VHL-E3 ubiquitin ligase

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

1

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-130604
    DT2216
    2 Publications Verification

    		 Bcl-2 Family PROTACs Apoptosis Cancer
    DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax-piperazine (HY-44432), a linker, and a VHL E3 ubiquitin ligase (Pink: Navitoclax-piperazine; Blue: VHL ligand; Black: linker) .
    DT2216
  • HY-160525
    NVS-VHL720

    		Molecular Glues Cancer
    NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer .
    NVS-VHL720
  • HY-173011
    RJS308

    		PROTACs Cyclophilin HIV HCV Infection
    RJS308 is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 exhibits anti-HIV-1 and anti-HCV activities. RJS308 can be used in studies related to viral infections .
    RJS308
  • HY-139218
    (S,R,S)-AHPC-Me-C6-NH2

    		E3 Ligase Ligand-Linker Conjugates Others
    (S,R,S)-AHPC-Me-C6-NH2 is a VHL E3 ubiquitin ligase ligand-linker conjugate structurally modified based on VHL ligand 2 (HY-112078). (S,R,S)-AHPC-Me-C6-NH2 can be used for the synthesis of PROTACs .
    (S,R,S)-AHPC-Me-C6-NH2
  • HY-128756
    SIAIS178

    		PROTACs Bcr-Abl Cancer
    SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity .
    SIAIS178
  • HY-173011A
    RJS308 TFA

    		PROTACs Cyclophilin HIV HCV Infection
    RJS308 TFA is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 TFA induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 TFA exhibits anti-HIV-1 and anti-HCV activities. RJS308 TFA can be used in studies related to viral infections .
    RJS308 TFA
  • HY-177119
    ZBP1 Covalent PROTAC-1

    		PROTACs RIP kinase Mixed Lineage Kinase Infection Inflammation/Immunology
    ZBP1 Covalent PROTAC-1 is a covalent Z-DNA binding protein 1 ZBP1 PROTAC degrader, with its DC50 being 25.69 nM. ZBP1 Covalent PROTAC-1 integrates the ligand that recruits the VHL E3 ubiquitin ligase and the DNA aptamer (Aptamer Z3) with the specific Zα domain that can bind to ZBP1, which has a high affinity (KD = 2.71 nM) with ZBP1. After degrading ZBP1, the phosphorylation levels of downstream signaling molecules RIPK3 and MLKL significantly decrease. ZBP1 Covalent PROTAC-1, encapsulated by nano-liposomes, significantly improves the survival rate of mice infected with influenza A virus (IAV) after administration via the trachea .
    ZBP1 Covalent PROTAC-1
  • HY-175358
    PROTAC USP7 Degrader-1

    		PROTACs Deubiquitinase Cancer
    PROTAC USP7 Degrader-1 is a VHL-recruiting PROTAC and USP7 degrader with binding activity to both USP7 and the VHL E3 ubiquitin ligase. PROTAC USP7 Degrader-1 recruits the VHL E3 ligase to mediate the ubiquitination and subsequent proteolytic degradation of USP7 .
    PROTAC USP7 Degrader-1
  • HY-122702
    PEG6-(CH2CO2H)2

    		PROTAC Linkers Others
    PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation .
    PEG6-(CH2CO2H)2
  • HY-P11493
    ALAPYIP

    		Ligands for E3 Ligase Cancer
    ALAPYIP is a ligand for E3 ligase. ALAPYIP recruits the VHL-E3 ubiquitin ligase. ALAPYIP can be used for the synthesis of FPP29 (HY-P11228) .
    ALAPYIP
  • HY-175025
    CH091138

    		PROTACs Ras Apoptosis Cancer
    CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .
    CH091138
  • HY-175885
    PROTAC FTO degrader 1

    		PROTACs Fat Mass and Obesity-associated Protein (FTO) Apoptosis Caspase PARP YTHDF Cancer
    PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML) . (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))
    PROTAC FTO degrader 1
  • HY-153321A
    (R,R)-Bexobrutideg

    (R,R)-NX-5948; (R,R)-BTK-IN-24

    		 Drug Isomer PROTACs Btk Inflammation/Immunology Cancer
    (R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    (R,R)-Bexobrutideg
  • HY-49514
    VHL Ligand intermediate-1

    		Ligands for E3 Ligase SOS1 Cancer
    VHL Ligand intermediate-1 (intermediate 18a) is an intermediate in the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .
    VHL Ligand intermediate-1
  • HY-49515
    VHL Ligand intermediate-2

    		Ligands for E3 Ligase SOS1 Cancer
    VHL Ligand intermediate-2 (compound 18c) is an intermediate for the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .
    VHL Ligand intermediate-2
  • HY-141651
    (S,R,S)-AHPC-C3-COOH

    		E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-C3-COOH (compound 28i) is a carboxylic acid derivative of the VHL E3 ubiquitin ligase ligand-Linker conjugate. (S,R,S)-AHPC-C3-COOH can be used to synthesize PROTACs .
    (S,R,S)-AHPC-C3-COOH
  • HY-181787
    DOT1L705

    		PROTACs Histone Methyltransferase Cardiovascular Disease
    DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia .
    DOT1L705
  • HY-181949
    PROTAC BRD9 Degrader-10

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD9 Degrader-10 is a PROTAC degrader targeting BRD9, with an IC50 of 2.97 μM against BRD9. PROTAC BRD9 Degrader-10 induces BRD9 degradation via the ubiquitin-proteasome system by recruiting the VHL E3 ubiquitin ligase. PROTAC BRD9 Degrader-10 reduces the viability and inhibits the proliferation of myeloid leukemia cells. PROTAC BRD9 Degrader-10 is applicable for the research of acute myeloid leukemia .
    PROTAC BRD9 Degrader-10
  • HY-183555
    MS108

    		PROTACs Epigenetic Reader Domain Cancer
    MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC50 of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog AF9, which shares a highly conserved YEATS domain with ENL. MS108 suppresses proliferation of cancer cells .
    MS108
  • HY-181728
    MS243

    		PROTACs Ras Cancer
    MS243 is a potent KRAS G12D PROTAC degrader with a DC50 of 4.2 nM. MS243 promotes the proximity between KRAS G12D and the VHL E3 ubiquitin ligase, drives the ubiquitination and proteasomal degradation of KRAS G12D, and inhibits the proliferation of cancer cells harboring KRAS G12D. MS243 can be used in the research of KRAS G12D-carrying cancers, such as colon cancer and pancreatic cancer .
    MS243
  • HY-183007
    LJM133

    		PROTACs SWI/SNF Complex Cancer
    LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC50 values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer . (Pink: SMARCA2/PBRM1/SMARCA4 ligand (HY-182987); E3 ubiquitin ligase ligand-linker conjugate (HY-183619)).
    LJM133
  • HY-183070
    CXJ2080

    		PROTACs CDK Apoptosis Cancer
    CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia .
    CXJ2080

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