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VHL+E3

" in MedChemExpress (MCE) Product Catalog:

56

Inhibitors & Agonists

1

Peptides

Cat. No. Nombre del producto Target Áreas de investigación 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-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-159607

    PROTACs SWI/SNF Complex Cancer
    PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
    PRT3789
  • 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-132296
    GSK215
    2 Publications Verification

    FAK PROTACs Cancer
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
    GSK215
  • HY-160525

    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

    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-171830

    YX39-105

    PROTACs Tyrosinase Apoptosis Cancer
    MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) (BRK) PROTAC degrader. MS105 recruits VHL E3 ligase via a VHL ligand moiety, promotes PTK6 ubiquitination and proteasomal degradation, inhibits the proliferation and migration of breast cancer cells, and induces apoptosis. MS105 shows potential for use in breast cancer research .
    MS105
  • HY-139218

    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-162362

    PROTACs GLP Receptor Cancer
    MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .
    MS8709
  • HY-158684

    PROTACs MDM-2/p53 Apoptosis Cancer
    YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity .
    YX-02-030
  • HY-160924

    PROTACs BMI1 E1/E2/E3 Enzyme Histone Methyltransferase Cancer
    MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma . (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)
    MS147
  • HY-128756

    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-133045

    Ligands for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
    VHL Ligand 8
  • HY-159779

    PROTACs Nuclear Hormone Receptor 4A/NR4A Inflammation/Immunology Cancer
    NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8 + T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer .
    NR-V04
  • HY-153598

    PROTACs RIP kinase Apoptosis Inflammation/Immunology Cancer
    LD4172 is a selective RIPK1 PROTAC degrader with a Ki of 4.8 nM. LD4172 induces RIPK1 protein degradation via ternary complex formation with RIPK1 and VHL E3 ligase, driving ubiquitination and proteasomal breakdown. LD4172 abrogates TNF-induced classical NF-κB signaling in TRAF2-deficient cells, impairing IκBα phosphorylation and degradation, and reducing IL-8 production. LD4172 induces apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy. LD4172 acts as a chemical probe for investigating RIPK1 scaffolding functions. LD4172 can be used for the research of melanoma, colon cancer .
    LD4172
  • HY-145819

    HDAC PROTACs Cancer
    JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS036
  • HY-173011A

    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-145816A
    JPS016 TFA
    1 Publications Verification

    HDAC PROTACs Apoptosis PINK1/Parkin Autophagy Reactive Oxygen Species (ROS) Cancer
    JPS016 TFA is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 TFA recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 TFA reduces the viability of colon cancer cells and induces Apoptosis. JPS016 TFA activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 TFA is applicable to research related to colon cancer and sepsis cardiomyopathy .
    JPS016 TFA
  • HY-177119

    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

    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

    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-145815A

    PROTACs HDAC Apoptosis Cancer
    JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS014 TFA
  • 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-175025

    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

    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-145818

    HDAC PROTACs Cancer
    JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS035
  • HY-145815

    HDAC PROTACs Cancer
    JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS014
  • HY-P11493

    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-145816

    PROTACs HDAC Apoptosis PINK1/Parkin Autophagy Reactive Oxygen Species (ROS) Cardiovascular Disease Cancer
    JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 reduces the viability of colon cancer cells and induces Apoptosis. JPS016 activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 is applicable to research related to colon cancer and sepsis cardiomyopathy .
    JPS016
  • HY-176823

    PROTACs SGK Cancer
    PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. (Pink: SGK3 ligand (HY-167701), Blue: VHL Ligand (HY-120217A), Black: Linker (HY-130618), SGK3 ligand-linker conjugate (HY-176824)) .
    PROTAC SGK3 degrader-2
  • HY-163845

    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-180907

    PROTACs Cancer
    PROTAC USP39 Degrader-1 (compound USP39_PROTAC_V1) is a potent and selective PROTAC USP39 degrader. PROTAC USP39 Degrader-1 induces degradation of USP39 by recruiting the VHL E3 ligase via a hydroxyl-proline-containing ligand, forming a ternary complex with a Kd of 232 nM. PROTAC USP39 Degrader-1 degrades USP39 in a VHL-, proteasome-, and the neddylation pathway-dependent manner .
    PROTAC USP39 Degrader-1
  • HY-159798

    PROTACs p38 MAPK Cancer
    NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)) .
    NR-11c
  • 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-153321A

    (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) [3].
    (R,R)-Bexobrutideg
  • HY-49514

    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

    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-164043

    Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC(Me)-amido-C2-acid is an VHL (E3 ligase) ligand, and can be used for synthesis of PROTACs, such as PROTAC STING Degrader-2 (HY-158036) .
    (S,R,S)-AHPC(Me)-amido-C2-acid
  • HY-148880

    Ligands for E3 Ligase Cancer
    VHLL-BCN is a ligand targeting the VHL E3 ligase, which can be used for the synthesis of PROTAC molecules. As a key component of the copper-free SPAAC-based rapid synthesis platform for transcription factor PROTACs, VHLL-BCN is applicable to cancer-related research .
    VHLL-BCN
  • HY-141651

    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-130642

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-Me-C10-Br is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-Me-C10-Br incorporates a VHL E3 ligase linker and MS432 based on the MEK1/2 inhibitor PD0325901 .
    (S,R,S)-AHPC-Me-C10-Br
  • HY-174856

    PROTACs HBV Infection
    PROTAC HBeAg degrader-1 is a PROTAC targeting degradation agent for HBeAg. PROTAC HBeAg degrader-1 recruits the VHL E3 ligase but degrades HBV protein HBeAg through VHL-independent mechanism. PROTAC HBeAg degrader-1 decreases levels of secreted and intracellular HBeAg. PROTAC HBeAg degrader-1 can be used for the research of hepatitis B virus (HBV) . (Structure Note: Pink: HBeAg ligand (HY-174857); Blue: VHL Ligand (HY-125845); Black: linker; E3-linker (HY-135045))
    PROTAC HBeAg degrader-1
  • HY-158429

    PROTACs Cytochrome P450 Cancer
    PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
    PROTAC CYP1B1 degrader-2
  • HY-160423

    PROTACs Histone Methyltransferase Cancer
    MS8815N is a negative control of EZH2 PROTAC degrader MS8815 (HY-148334). MS8815N is incapable of recruiting the VHL E3 ligase but retains the same EZH2 binding moiety and linker. MS8815N can be used for triple-negative breast cancer (TNBC) research .
    MS8815N
  • HY-181787

    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-183555

    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

    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-181949

    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-186146A

    SGI-1776-cis-VHL-02

    Drug Isomer Pim c-Myc Apoptosis Cancer
    SGI-1776-VHL-02-epimer (SGI-1776-cis-VHL-02) is an epimer control compound of with SGI-1776-VHL-02 (HY-186146). SGI-1776-VHL-02-epimer has an inverted stereocenter in the critical hydroxyl-proline group in the VHL ligand. SGI-1776-VHL-02-epimer cannot trigger the VHL E3 ligase complex and does not degrade PIM1 .
    SGI-1776-VHL-02-epimer

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