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Targeted Degradation

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-11103
    Sitaxsentan sodium
    2 Publications Verification

    IPI 1040 sodium; TBC11251 sodium

    		 Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan sodium
  • HY-163640
    CDK4 degrader 1

    		Molecular Glues CDK Cancer
    CDK4 degrader 1 (ML 1–71) is a molecular glue degrader that targets CDK4 .
    CDK4 degrader 1
  • 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-112557
    PROTAC TBK1 degrader-2
    1 Publications Verification

    		 PROTACs IKK Cancer
    PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM) .
    PROTAC TBK1 degrader-2
  • HY-141881
    PROTAC-O4I2

    		PROTACs Apoptosis SF3B1 Cancer
    PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells .
    PROTAC-O4I2
  • HY-130615
    PROTAC EED degrader-2
    1 Publications Verification

    		 PROTACs Histone Methyltransferase Cancer
    PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit .
    PROTAC EED degrader-2
  • HY-163638
    BRD4 degrader-1

    		Epigenetic Reader Domain Molecular Glues E1/E2/E3 Enzyme Cancer
    BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research .
    BRD4 degrader-1
  • HY-158142
    PROTAC TYK2 degrader-1

    		PROTACs JAK Inflammation/Immunology Cancer
    PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%.
    PROTAC TYK2 degrader-1
  • HY-168624
    VAV1 degrader-2

    		Molecular Glues Inflammation/Immunology
    VAV1 degrader-2 is a molecular glue degrader based on targeting Vav guanine nucleotide exchange factor 1 (VAV 1) with a DC50 of 4.41 nM. VAV1 degrader-2 can be used in the study of inflammatory and autoimmune diseases .
    VAV1 degrader-2
  • HY-146324
    PROTAC eEF2K degrader-1

    		PROTACs Apoptosis CaMK Cancer
    PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation .
    PROTAC eEF2K degrader-1
  • HY-161108
    PROTAC Chk1 degrader-1

    		PROTACs Checkpoint Kinase (Chk) Cancer
    PROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma .
    PROTAC Chk1 degrader-1
  • 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-130614
    PROTAC EED degrader-1

    		PROTACs Histone Methyltransferase Cancer
    PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit .
    PROTAC EED degrader-1
  • HY-134592
    Piperidine-GNE-049-N-Boc

    		Ligands for Target Protein for PROTAC Cancer
    Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP .
    Piperidine-GNE-049-N-Boc
  • HY-P11498
    Cyclomarin monomer-2

    		Drug Intermediate Bacterial Infection
    Cyclomarin monomer-2 (Compound 10), a cyclomarin monomer, is a pre-dimerization precursor that can form Homo-BacPROTACs targeting the degradation of ClpC1. Cyclomarin monomer-2 binds to the Mtb ClpC1 protein with a KD of 4.0 nM. The MIC of Cyclomarin monomer-2 against the Mtb H37Rv standard strain is 3.1 μM. Cyclomarin monomer-2 can be used as a key intermediate in the development of Homo-BacPROTACs .
    Cyclomarin monomer-2
  • HY-168037
    PROTAC PIN1 degrader-1

    		PROTACs PIN1 Cancer
    PROTAC PIN1 degrader-1 is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer .
    PROTAC PIN1 degrader-1
  • HY-156566
    PROTAC BRD4 Degrader-21

    		PROTACs Epigenetic Reader Domain HSP Cancer
    PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .
    PROTAC BRD4 Degrader-21
  • HY-169343
    FIZ1 degrader 1

    		Molecular Glues Cancer
    FIZ1 degrader 1 (compound 1) is an IMiD-based molecular glue degrader targeting FIZ1 .
    FIZ1 degrader 1
  • HY-157512
    SJF-0661

    		Ligands for E3 Ligase Cancer
    SJF-0661 is a variant of the von Hippel-Lindau (VHL) protein ligand with no targeted degradation ability and can be used as a control reagent for the VHL ubiquitin ligase ligand. SJF-0661 is a variant obtained by inverting the stereocenter of the key hydroxyproline group in the VHL ligand .
    SJF-0661
  • HY-157213
    LWY713

    		Apoptosis PROTACs FLT3 Cancer
    LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
    LWY713
  • HY-P11497
    Cyclomarin monomer-1

    		Drug Intermediate Bacterial Infection
    Cyclomarin monomer-1 (Compound 5), a cyclomarin monomer, is a pre-dimerization precursor that can form Homo-BacPROTACs targeting the degradation of ClpC1. Cyclomarin monomer-1 binds to the Mtb ClpC1 protein with a KD of 3.5 nM. The MIC of Cyclomarin monomer-1 against the Mtb H37Rv standard strain is 1.6 μM. Cyclomarin monomer-1 can be used as a key intermediate in the development of Homo-BacPROTACs .
    Cyclomarin monomer-1
  • HY-115728
    PROTAC CDK9 degrader-4

    		PROTACs Cancer
    PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.
    PROTAC CDK9 degrader-4
  • HY-152145
    PROTAC SOS1 degrader-3

    		SOS1 PROTACs Ras Cancer
    PROTAC SOS1 degrader-3 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-3 effectively targeted SOS1 for degradation through the ubiquitin-proteasome system .
    PROTAC SOS1 degrader-3
  • HY-161795
    SP3CHO

    		Drug Metabolite Cancer
    SP3CHO is an active metabolite generated by the metabolism of SP3N in cell culture by the action of amine oxidase. SP3CHO can induce polyubiquitination of specific proteins by recruiting the SCFFBXO22 E3 ligase complex. SP3CHO can be used in cancer therapy research .
    SP3CHO
  • HY-149964
    PROTAC CDK9 degrader-7

    		PROTACs CDK Cancer
    PROTAC CDK9 degrader-7 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-7 mediates CDK9 degradation via the proteasome .
    PROTAC CDK9 degrader-7
  • HY-174238
    GSPT1 degrader-7

    		Molecular Glues Cancer
    GSPT1 degrader-7 (Example 43) is a molecular glue degrader targeting GSPT1. GSPT1 degrader-7 has an EC50 of 0.2 nM in DF15 multiple myeloma cells. GSPT1 degrader-7 can be used in the study of cancer .
    GSPT1 degrader-7
  • HY-175975
    PROTAC Akt3 Degrader-1

    		PROTACs Akt Cancer
    PROTAC Akt3 Degrader-1 is a highly efficient and selective PROTAC degrader targeting Akt3. PROTAC Akt3 Degrader-1 shows weak antiproliferative activity in 36 cell lines. PROTAC Akt3 Degrader-1 can be used for the study of Triple-negative breast cancer and melanoma .
    PROTAC Akt3 Degrader-1
  • HY-175280
    Lck degrader-1

    		Molecular Glues Src Cancer
    Lck degrader-1 (Compound 17) is a molecular glue degrader targeting lymphocyte-specific protein tyrosine kinase (LCK) (DC50=23.1 nM). Lck degrader-1 is promising for research of T-cell acute lymphoblastic leukemia (T-ALL) .
    Lck degrader-1
  • HY-176261
    DDD2

    		PROTACs Cancer
    DDD2 is a selective and potent VHL-mediated PROTAC NUDT5 degrader. DDD2 induces robust NUDT5 degradation. DDD2 can be used in cancer research, such as lymphocytic leukemia and osteosarcoma . (Structure Note: Pink: NUDT5 inhibitor (HY-176262); Blue: E3 (HY-125845); Black: linker (HY-W001958))
    DDD2
  • HY-174225
    sEH-H ligand 1

    		Ligands for Target Protein for PROTAC Epoxide Hydrolase Others
    sEH-H ligand 1 is a PROTAC target protein ligand that can be used to synthesize PROTAC sEH degrader-2 (HY-174443) .
    sEH-H ligand 1
  • HY-174877
    PROTAC HDAC6 degrader 6

    		PROTACs HDAC Cancer
    PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ∼50% Dmax only upon activation to its cis-state with 390 nm light irradiation . Pink: HDAC6 ligand; Blue: CRBN ligase ligand (HY-A0003); Black: linker
    PROTAC HDAC6 degrader 6
  • HY-162411
    E3 ligase Ligand 24

    		Ligands for E3 Ligase Cancer
    E3 ligase Ligand 24 (Compound 24) is a Potent Ligand for the E3 Ligase DCAF15 (IC50= 0.053 μM). Due to E3 ligase Ligand 24’s selectivity and potent binding characteristics, it is pivotal in the study of targeted protein degradation .
    E3 ligase Ligand 24
  • HY-175144
    KRASG12D-IN-6

    		Ligands for Target Protein for PROTAC Ras Cancer
    KRASG12D-IN-6 is a PROTAC target protein ligand that can be used to synthesize CH091138 (HY-175025). CH091138 is a potent and selective KRASG12D PROTAC degrader with anti-tumor activity .
    KRASG12D-IN-6
  • HY-134725
    MTH1 degrader-1

    		DNA/RNA Synthesis Ligands for Target Protein for PROTAC Cancer
    MTH1 degrader-1, a MTH1 aTAG inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). MTH1 degrader-1 can be used for synthesis PROTAC aTAG 4531 (HY-163168) .
    MTH1 degrader-1
  • HY-159894
    Autophagy-lysosome activator-1

    		Autophagy Cancer
    Autophagy-lysosome activator-1 (Compound F1) is a Autophagy-lysosome activator. Autophagy-lysosome activator-1 effectively induces PD-L1 or VISTA degradation in tumor cells .
    Autophagy-lysosome activator-1
  • HY-177729
    PROTAC BRD9 Degrader-9

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD9 Degrader-9 (Compound 16) is an efficient and selective targeting BRD9 PROTAC degrader. PROTAC BRD9 Degrader-9 does not cause significant cytotoxicity. PROTAC BRD9 Degrader-9 can be used for cancer research
    PROTAC BRD9 Degrader-9
  • HY-168017
    NSC682769

    		Ligands for Target Protein for PROTAC YAP Cancer
    NSC682769 is a PROTAC YAP-targeting ligand (Ligands for Target Protein for PROTACs). NSC682769 can be used for synthesis PROTAC YAP degrader-1 (HY-168016) .
    NSC682769
  • HY-146422
    PROTAC EGFR degrader 5

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .
    PROTAC EGFR degrader 5
  • HY-146423
    PROTAC EGFR degrader 6

    		PROTACs EGFR Apoptosis Cancer
    PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .
    PROTAC EGFR degrader 6
  • HY-170341
    ER ligand-6

    		Ligands for Target Protein for PROTAC Estrogen Receptor/ERR Cancer
    ER ligand-6 is a target protein ligand of PROTAC ER Degrader-14 (HY-170340) .
    ER ligand-6
  • HY-149962
    PROTAC CDK9 degrader-5

    		PROTACs CDK Cancer
    PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively .
    PROTAC CDK9 degrader-5
  • HY-141486A
    PROTAC PARP/EGFR ligand 1

    		PARP EGFR Ligands for Target Protein for PROTAC Others
    PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology .
    PROTAC PARP/EGFR ligand 1
  • HY-168702
    FLT3 ligand-2

    		Ligands for Target Protein for PROTAC Cancer
    FLT3 ligand-2 is a Ligand for Target Protein for PROTAC. FLT3 ligand-2 can be used to synthesize PROTAC FLT-3 degrader 1 (HY-114323) .
    FLT3 ligand-2
  • HY-145947
    PROTAC BRD9 Degrader-5

    		PROTACs Cancer
    PROTAC BRD9 Degrader-5 is a PROTAC for targeted degradation of BRD9.
    PROTAC BRD9 Degrader-5
  • HY-168055
    (S)-Deoxy-thalidomide

    		Ligands for E3 Ligase Cancer
    (S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation .
    (S)-Deoxy-thalidomide
  • HY-173369
    PROTAC MAGL degrader-1

    		PROTACs MAGL Cancer
    PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249) .
    PROTAC MAGL degrader-1
  • HY-149679
    PROTAC eDHFR Degrader-2

    		PROTACs Bacterial Cancer
    PROTAC eDHFR Degrader-2 (compound 7b) is a potent degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), enabling robust degradation of eDHFR-tagged proteins .
    PROTAC eDHFR Degrader-2
  • HY-168056
    KRAS ligand 5

    		Ligands for Target Protein for PROTAC Ras Others
    KRAS ligand 5 is the target protein ligand for PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can specifically degrade KRAS mutated proteins .
    KRAS ligand 5
  • HY-173372
    PROTAC AR Degrader-10

    		Androgen Receptor PROTACs Cancer
    PROTAC AR Degrader-10 (GT19) is a protein degrader targeting the androgen receptor (AR) with a DC50 value ≤100 nM. PROTAC AR Degrader-10 can be used for prostate cancer study. (Structure Note: Pink: target protein ligand (HY-173373); Blue: E3 ligase ligand (HY-138793); Black: linker) .
    PROTAC AR Degrader-10
  • HY-159662
    HSD17B13 degrader 2

    		Ligands for Target Protein for PROTAC Cancer
    HSD17B13 degrader 2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). HSD17B13 degrader 2 can be used for synthesis PTOTAC HSD17B13 degrader 1 (HY-159651) .
    HSD17B13 degrader 2

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