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Pathways Recommended: MAPK/ERK Pathway
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ubiquitin pathway

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100487
    TAK-243
    Maximum Cited Publications
    83 Publications Verification

    MLN7243

    E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .
    TAK-243
  • HY-141432

    Cbl-b-IN-3

    E1/E2/E3 Enzyme Cancer
    NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research .
    NX-1607
  • HY-145449

    E3 Ligase Ligand-Linker Conjugates ADC Payload Cancer
    CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC). CC-885-CH2-PEG1-NH-CH3 is the toxic molecule of ADC, which can specifically degrade the target protein in cancer cells through the E3 ubiquitin ligase pathway .
    CC-885-CH2-PEG1-NH-CH3
  • HY-157228

    PROTACs Ras Cancer
    ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
    ACBI3
  • HY-145898

    14-D-Valine-TPL

    c-Myc Molecular Glues Cancer
    WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .
    WBC100
  • HY-150505
    DC-U4106
    1 Publications Verification

    Deubiquitinase Apoptosis Cancer
    DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer .
    DC-U4106
  • HY-144841

    CFT7455

    Molecular Glues IKZF Family Cancer
    Cemsidomide (CFT7455) is a ubiquitin ligase pathway based IKZF1/3 (Ikaros/Aiolos) degrader with molecular glue activity . Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells. Cemsidomide is used in the research of multiple myeloma (MM) .
    Cemsidomide
  • HY-P10899

    PROTACs TGF-beta/Smad Endocrinology
    ETTAC-2 is a LRG1 PROTAC degrader, degrading LRG1 via the ubiquitin-proteasome pathway with a DC50 value of 8.38 μM. ETTAC-2 penetrates damaged renal cells to reduce the extracellular secretion of LRG1. ETTAC-2 effectively inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated extracellular matrix proteins. ETTAC-2 degrades LRG1 within fibrotic kidneys and the efficacy in inhibiting the TGF-β-Smad3 pathway both in vitro and vivo. ETTAC-2 can be used for renal fibrosis research .
    ETTAC-2
  • HY-13811
    NSC697923
    5+ Cited Publications

    E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
    NSC697923
  • HY-19726
    NSC59984
    2 Publications Verification

    MDM-2/p53 Cancer
    NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling .
    NSC59984
  • HY-12842

    IAP Survivin Apoptosis Caspase Inflammation/Immunology Cancer
    UC-112 is a XIAP inhibitor with anticancer activity. UC-112 selectively downregulates and degrades survivin via the ubiquitin-mediated proteasomal degradation pathway. UC-112 reduces XIAP levels in in vivo tumor models. UC-112 activates caspase-3/7 and caspase-9, and induces cancer cell apoptosis. UC-112 is applicable to studies on melanoma, prostate cancer and cancer-related research .
    UC-112
  • HY-136242

    Estrogen Receptor/ERR Endocrinology Cancer
    UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
    UT-34
  • HY-149760

    PROTACs Phosphatase IFNAR STAT Cancer
    PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma . (Pink: PTPN2 ligand (HY-168691), Black: linker (HY-B0236), Blue: VHL ligand (HY-112078)).
    PVD-06
  • HY-N10549
    Gigantol
    1 Publications Verification

    Ferroptosis c-Myc Glutathione Peroxidase JNK Reactive Oxygen Species (ROS) GSK-3 Infection Metabolic Disease Cancer
    Gigantol is an orally active bibenzyl compound. Gigantol targets MYC to promote its ubiquitin-proteasomal degradation and inhibit the growth of lung cancer cells. Gigantol exerts anti-lung cancer activity by inducing ferroptosis (Ferroptosis) via the SLC7A11-GPX4 axis. Gigantol restores the sensitivity of mcr-harboring multidrug-resistant bacteria to colistin. Gigantol ameliorates carbon tetrachloride-induced liver injury by inhibiting the activation of the JNK/cPLA2/12-LOX inflammatory pathway. Gigantol promotes cholesterol metabolism and progesterone biosynthesis in Leydig cells. Gigantol can be used in studies related to diseases such as lung cancer, multidrug-resistant Gram-negative bacterial infections, and acute liver injury .
    Gigantol
  • HY-152134

    HDAC PROTACs Cancer
    HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin .
    HDAC6 degrader-3
  • HY-173351

    Epigenetic Reader Domain Cancer
    G-6599 is a monovalent molecular glue-like degrader of SMARCA2/SMARCA4. G-6599 covalently binds to a specific cysteine residue of the E3 ligase FBXO22 in a biotransformation-independent manner, promotes the formation of a ternary complex with SMARCA2/A4, and achieves efficient and specific degradation of the two proteins via the ubiquitin-proteasome pathway. G-6599 is applicable to the research of androgen-dependent prostate cancer and mutant non-small cell lung cancer .
    G-6599
  • HY-125834

    PROTACs Bcr-Abl Apoptosis STAT JAK Cancer
    GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
    GMB-475
  • HY-162562

    PCSK9 Metabolic Disease Inflammation/Immunology
    E28362 is an orally active lipid-lowering agent and a selective PCSK9 antagonist. E28362 blocks the interaction between PCSK9 and LDLR, and induces PCSK9 degradation via the ubiquitin-proteasome pathway. E28362 significantly increases the levels of cell surface and total LDLR proteins, enhances low-density lipoprotein uptake, thereby effectively reducing plasma lipids, hepatic cholesterol and triglyceride levels. E28362 shows no obvious cytotoxicity at high concentrations, and significantly attenuates atherosclerotic lesions in animal models. E28362 is an important molecule in research of hyperlipidemia and atherosclerosis .
    E28362
  • HY-P11228

    PROTACs Apoptosis DNA/RNA Synthesis Cancer
    FPP29 is a potent peptide-based FOXM1 PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)) .
    FPP29
  • HY-149127

    ASC-JM17; ALZ-003

    Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy Metabolic Disease
    Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .
    Rosolutamide
  • HY-W181530

    Molecular Glues CDK Apoptosis Ligands for E3 Ligase Cancer
    NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
    NCT02
  • HY-137341

    PROTACs YTHDF Cancer
    SK-3-91 is a PROTAC-type multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). SK-3-91 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway. SK-3-91 degrades YTHDF2. SK-3-91 inhibits cell proliferation and induces morphological changes. (Pink: TAE648 ligand (HY-169396); Blue: E3 ligase ligand (HY-131717); Black: Linker (HY-140819). The E3 ligase ligand and linker can form a conjugate (HY-169397)) .
    SK-3-91
  • HY-175839

    PROTACs EGFR ATP Synthase Cancer
    PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
    PROTAC EGFR degrader 15
  • HY-111876

    SNIPERs Cancer
    SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-1 induces cancer cell death .
    SNIPER(TACC3)-1
  • HY-N7695

    Apoptosis Autophagy Cancer
    Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
    Physalin B
  • HY-158345

    PROTACs ATM/ATR DNA/RNA Synthesis Apoptosis Cancer
    PROTAC ATM degrader-1 is a ATM PROTAC degrader with a KD value of 1.17 nM. PROTAC ATM degrader-1 triggers DNA damage response, cell cycle arrest, and apoptosis in cancer cells via the ubiquitin-proteasome-dependent degradation pathway. PROTAC ATM degrader-1 can be used for research on colorectal cancer .
    PROTAC ATM degrader-1
  • HY-153896
    LMTK3-IN-1
    1 Publications Verification

    c-Met/HGFR Cancer
    LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM),that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
    LMTK3-IN-1
  • HY-173414

    PROTACs STING NF-κB Inflammation/Immunology
    PROTAC STING degrader-3 is a STING PROTAC degrader (DC50: 0.62 μM). PROTAC STING degrader-3 induces STING degradation via the ubiquitin-proteasome pathway. PROTAC STING degrader-3 exerts anti-inflammatory effects by inhibiting STING/TBK1/NF-κB signaling. PROTAC STING degrader-3 has renal protective effects and can be used in the study of acute kidney injury (AKI) .
    PROTAC STING degrader-3
  • HY-158432

    Histone Demethylase PROTACs Cancer
    GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
    GT-653
  • HY-162749A

    PROTACs Histone Methyltransferase Apoptosis Cancer
    G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer .
    G9D-4 TFA
  • HY-170859

    PROTACs Casein Kinase Cancer
    AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma .
    AH078
  • HY-175764

    PROTACs IRAK NF-κB p38 MAPK TNF Receptor Interleukin Related Inflammation/Immunology
    FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)) .
    FIP22
  • HY-103435
    Vialinin A
    2 Publications Verification

    Terrestrin A

    Deubiquitinase TNF Receptor E1/E2/E3 Enzyme Keap1-Nrf2 Inflammation/Immunology Cancer
    Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke .
    Vialinin A
  • HY-111877

    SNIPERs Cancer
    SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-2 induces cancer cell death .
    SNIPER(TACC3)-2
  • HY-147942

    PROTACs EGFR Cancer
    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
    MS9449
  • HY-147941

    PROTACs EGFR Inflammation/Immunology Cancer
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
    MS9427
  • HY-P1259A

    Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
    PR-39 TFA
  • HY-174416

    E1/E2/E3 Enzyme Cardiovascular Disease
    Smurf1-IN-5 (Compound cpd-6) is an allosteric SMAD ubiquitin regulatory factor 1 (SMURF1) inhibitor. Smurf1-IN-5 leads to a reduction in the ubiquitylation of substrates such as BMPR2 (bone morphogenetic protein receptor 2) and SMAD1, enhancing the BMP (bone morphogenetic protein) signaling pathway. Smurf1-IN-5 is promising for research of pulmonary arterial hypertension (PAH) .
    Smurf1-IN-5
  • HY-145449A

    E3 Ligase Ligand-Linker Conjugates ADC Payload Cancer
    CC-885-CH2-PEG1-NH-CH3 TFA is a new degrader that can be used to synthesize antibody-based novel degrader conjugated active molecules (AnDC). CC-885-CH2-PEG1-NH-CH3 TFA is the toxic molecule of ADC, which can specifically degrade the target protein in cancer cells through the E3 ubiquitin ligase pathway .
    CC-885-CH2-PEG1-NH-CH3 TFA
  • HY-174428

    PROTACs JAK STAT Apoptosis Cancer
    PROTAC JAK2 degrader-1 is a JAK2 PROTAC degrader, with a DC50 of 27.35 nM. PROTAC JAK2 degrader-1 induces JAK2 degradation via the ubiquitin-proteasome pathway. PROTAC JAK2 degrader-1 inhibits the JAK2-STAT signaling pathway. PROTAC JAK2 degrader-1 induces G2/M phase arrest and apoptosis in cancer cells. PROTAC JAK2 degrader-1 exhibits antiproliferative activity against cancer cells. PROTAC JAK2 degrader-1 inhibits recombinant human erythropoietin (rhEPO)-mediated polycythemia and splenomegaly in mice. PROTAC JAK2 degrader-1 can be used for research on myeloproliferative neoplasms, including polycythemia vera .
    PROTAC JAK2 degrader-1
  • HY-162749

    PROTACs Histone Methyltransferase Apoptosis Cancer
    G9D-4 is a G9a PROTAC degrader. G9D-4 induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 can be used for research on pancreatic cancer .
    G9D-4
  • HY-176184

    PROTACs Discoidin Domain Receptor MMP Cancer
    PROTAC DDR1 degrader-1 is a potent and selective DDR1-targeting PROTAC degrader. PROTAC DDR1 degrader-1 selectively induces full-length DDR1 degradation via the ubiquitin proteasome system, blocking downstream signaling pathways. PROTAC DDR1 degrader-1 inhibits tumor cell migration and invasion. PROTAC DDR1 degrader-1 exhibits anti-tumor activity in mice. PROTAC DDR1 degrader-1 can be used for the research of DDR1-driven cancers .
    PROTAC DDR1 degrader-1
  • HY-159728

    PROTACs Histone Methyltransferase Apoptosis Early 2 Factor (E2F) c-Myc Cancer
    PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia .
    PROTAC PRMT3 degrader 1
  • HY-153322

    PROTACs Itk Inflammation/Immunology Cancer
    ITK degrader 2 is an orally active ITK PROTAC degrader with a DC50 < 0.001 nM. ITK degrader 2 degrades ITK via the ubiquitin-proteasome pathway. ITK degrader 2 can be used in the research of cancer, autoimmune diseases and inflammatory diseases .
    ITK degrader 2
  • HY-173002

    DNA Methyltransferase Cancer
    MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
    MS9024
  • HY-179243

    PROTACs STAT MDM-2/p53 Cancer
    S3D5 is a highly efficient and selective PROTAC degrader targeting STAT3 (KD = 4.35 μM). S3D5 induces degradation of STAT3 in HepG2 cells without significant effects on other STAT proteins. S3D5 exhibits good anti-hepatocellular carcinoma cell proliferation activity, which can be explained by activating the p53 pathway. S3D5 degradation of the STAT3 protein is mediated by the ubiquitin–proteasome system (UPS). S3D5 can be used for the study of hepatocellular carcinoma .
    S3D5
  • HY-137340

    PROTACs Casein Kinase Cancer
    WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647) .
    WH-10417-099
  • HY-173097

    VH032-Boc derivative 1

    MALT1 Cancer
    (S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1, leading to ubiquitination and subsequent proteasomal degradation of MALT1. (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway by disrupting the CBM complex, demonstrating potential for inducing apoptosis in ABC-DLBCL cells. (S,R,S)-AHPC-Boc derivative 1 is promising for research of MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL) .
    (S,R,S)-AHPC-Boc derivative 1
  • HY-179035

    Molecular Glues CXCR Cancer
    TBS6b is a potent and selective ACKR3 molecular glue degrader. TBS6b degrades ACKR3 via the ubiquitin-proteasome pathway. TBS6b inhibits hepatocellular carcinoma cell proliferation, migration, and invasion. TBS6b is relevant to hepatocellular carcinoma (HCC) research .
    TBS6b
  • HY-P1259

    Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
    PR-39

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