Search Result
Results for "
MG degrader1
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
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Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-163897
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PROTACs
Ferroptosis
Reactive Oxygen Species (ROS)
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Inflammation/Immunology
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PROTAC NCOA4 degrader-1 is a VHL-based PROTAC NCOA4 degrader. PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces Fe 2+ elevation, ROS production, MDA content and PTGS2 mRNA expression. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. PROTAC NCOA4 degrader-1 can be used for the researches of inflammation and immunology. (Pink: NCOA4 ligand (HY-149457). Black: linker (HY-163903). Blue: VHL ligand (HY-138678B)) .
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- HY-176857
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PROTACs
STAT
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Inflammation/Immunology
Cancer
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PROTAC STAT6 degrader-1 (Compound I-2) is a potent STAT6 PROTAC degrader with a DC50 <1 nM. PROTAC STAT6 degrader-1 inhibits STAT6 activity with an IC50 of <0.1 pM. PROTAC STAT6 degrader-1 can be used for inflammatory and cancers research, such as non-small cell lung cancer (NSCLC) .
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- HY-168016
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PROTACs
YAP
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Cancer
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PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma .
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- HY-163638
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Epigenetic Reader Domain
Molecular Glues
E1/E2/E3 Enzyme
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Cancer
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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 .
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- HY-176528
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ERK
PROTACs
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Cancer
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PROTAC ERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. PROTAC ERK5 degrader-1 induces ERK5 degradation via VHL-mediated proteasome pathway in MOLT-4 cells. PROTAC ERK5 degrader-1 can be used for the study of a disease or disorder characterized by aberrant ERK5 activity, such as acute lymphoblastic leukemia .
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- HY-158342
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PROTACs
YAP
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Cancer
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PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .
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- HY-148691
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Phosphatase
PROTACs
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Metabolic Disease
Cancer
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PROTAC PTPN2 degrader-1 (compound example 77) is a potent PTPN2 degrader. PROTAC PTPN2 degrader-1 has the potential for the research of cancer or metabolic disease .
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- HY-173320
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Hsp-targeting Chimeras
Wee1
HSP
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Cancer
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HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
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- HY-158142
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PROTACs
JAK
STAT
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Inflammation/Immunology
Cancer
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PROTAC TYK2 degrader-1 is a TYK2 PROTAC degrader with a Dmax ≥ 60%. PROTAC TYK2 degrader-1 reduces the phosphorylation levels of IFNα-induced STAT1 (Tyr701) and STAT3 (Tyr705) in immune cells. PROTAC TYK2 degrader-1 can be used in research on cancer, inflammatory diseases, etc.
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- HY-158045
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PROTACs
PARP
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Cancer
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PROTAC PARP1 degrader-1 is a PARP1 PROTAC degrader with a DC50 value of 252.5 nM. PROTAC PARP1 degrader-1, combined with Daunorubicin (HY-13062A), induces the accumulation of cytoplasmic DNA fragments, activates the cGAS/STING innate immune pathway, and remodels the tumor microenvironment. PROTAC PARP1 degrader-1 can be used in research related to breast cancer .
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- HY-129523
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PROTACs
Ras
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Cancer
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PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells .
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- HY-153864
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PROTACs
MEK
ERK
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Cancer
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PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
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- HY-161108
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PROTACs
Checkpoint Kinase (Chk)
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Cancer
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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 .
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- HY-158345
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PROTACs
ATM/ATR
DNA/RNA Synthesis
Apoptosis
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Cancer
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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 .
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- HY-153415
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PROTACs
Bcr-Abl
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Cancer
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PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer .
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- HY-142662A
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PROTACs
IRAK
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Others
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PROTAC IRAK3 degrader-1 formic is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 formic induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 formic can be used for cancer research .
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- HY-163372
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PROTACs
MAP4K
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Cancer
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PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with DC50 value of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits phosphorylation of the SLP76 protein with IC50 value of 496.1 nM. PROTAC HPK1 Degrader-1 is a bona fide HPK1-PROTAC degrader, which provided a potential tool for further HPK1 investigation in TCR signaling .
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- HY-161101
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PROTACs
IKZF Family
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Cancer
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MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC50 value of 1.385 nM in MM.1S cells .
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- HY-168530
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PD-1/PD-L1
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Cancer
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PDL1 degrader-1 (compound PMT-O9-1A) is a potent PD-L1 degrader. PDL1 degrader-1 decreases the protein expression of PD-L1. PDL1 degrader-1 shows cytotoxicity. PDL1 degrader-1 shows anticancer activity .
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- HY-174428
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PROTACs
JAK
STAT
Apoptosis
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Cancer
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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 .
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- HY-156152A
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PROTACs
Histone Methyltransferase
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Cancer
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CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research .
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- HY-168135
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PROTACs
c-Met/HGFR
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Cancer
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PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer .
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- HY-145159
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SHP2
PROTACs
Phosphatase
Apoptosis
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Cancer
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SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases .
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- HY-176184
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PROTACs
Discoidin Domain Receptor
MMP
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Cancer
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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 .
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- HY-155552
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Apoptosis
CDK
Caspase
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Cancer
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GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G0/G1 phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research .
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- HY-147108
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Mitochondrial Metabolism
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Mitochondria degrader-1 (example 5) is a potent mitochondria degrader. Mitochondria degrader-1 induces the degradation of the injured mitochondria by the autophagy mechanism. Mitochondria degrader-1 can be used for the research of neurodegenerative disease, cancer, inflammatory disease, age-related disease, metabolic disease, mitochondrial disease or Down's disease .
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- HY-145737A
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Ras
PROTACs
SOS1
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Cancer
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PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
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- HY-112098
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
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- HY-163295
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ADC Payload
Btk
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Cancer
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BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect .
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- HY-160115
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DNA/RNA Synthesis
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Neurological Disease
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TDP-43 degrader-1 (Compound example 7) is a TDP-43 degrader. TDP-43 degrader-1 reduces the aggregation of TDP-43-positive HuR stress granules in cells and promotes the relocalization of abnormally distributed TDP-43 in the cytoplasm to the nucleus. TDP-43 degrader-1 can be used in the study of amyotrophic lateral sclerosis and Alzheimer's disease .
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- HY-158985A
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Autophagy
AUTACs
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Cancer
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Amino-PEG3-2G degrader-1 hydrochloride is the hydrochloride salt form of Amino-PEG3-2G degrader-1 (HY-158985). Amino-PEG3-2G degrader-1 hydrochloride is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 hydrochloride can be used to synthesize autophagy-targeting chimeras (AUTACs) .
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- HY-142662
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PROTACs
IRAK
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Cancer
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PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research .
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- HY-160532
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Casein Kinase
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Cancer
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CK1α degrader-1 (Compound 82) is an orally active CK1α degrader with a DC50 of 0.105 μM. CK1α degrader-1 can be used for the research of cancer .
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- HY-157216
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HDAC
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Cancer
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HDAC1 Degrader-1 (compound 1a) is an HDAC1 degrader with anticancer activity. HDAC1 Degrader-1 significantly reduces HDAC1 levels in MM.1S multiple myeloma cells .
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- HY-168037
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PROTACs
PIN1
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Cancer
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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 .
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- HY-133696
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PROTAC Linkers
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Cancer
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Tert-Butyl 8-hydroxyoctanoate is a PROTAC linker that can be used for the synthesis of PROTACs, such as PROTAC CDK Degrader-1 (HY-133617). PROTAC CDK Degrader-1 is a potent CDK PROTAC degrader with anti-tumor activity .
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- HY-163641
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Molecular Glues
Androgen Receptor
E1/E2/E3 Enzyme
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Cancer
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AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells .
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- HY-156152
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PROTACs
Histone Methyltransferase
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Cancer
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CARM1 degrader-1 is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer .
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- HY-145737
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PROTACs
SOS1
Ras
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Cancer
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PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
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- HY-175975
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PROTACs
Akt
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Cancer
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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 .
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- HY-147048
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STAT
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Cancer
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STAT3 degrader-1 (compound 295) is a potent STAT3 degrader. STAT3 degrader-1 can be used for researching anticancer . STAT3 degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-153424
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Target Protein Ligand-Linker Conjugates
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Cancer
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PROTAC SMARCA2 degrader-1 (compound ex7) is a BRM2 (SMARCA2) degrader (DC50<0.1 μM). PROTAC SMARCA2 degrader-1 is also an E3 ubiquitin ligase binding linker useful in research of cancers. PROTAC SMARCA2 degrader-1 is a target protein ligand-linker conjugate .
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- HY-144657A
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PROTACs
Ras
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Cancer
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(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .
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- HY-162014
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PROTACs
WDR5
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Cancer
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WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .
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- HY-128838
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader .
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- HY-164895
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PIN1
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Cancer
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PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research .
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- HY-176526
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Drug Intermediate
Btk
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Cancer
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BTK degrader-1 intermediate (compound 5) is an intermediate for the synthesis of BTK degrader-1 (HY-163295). BTK degrader-1 can be used as an ADC toxin to synthesize antibody-drug conjugate (ADC) .
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- HY-170601
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PROTACs
JNK
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Inflammation/Immunology
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PROTAC JNK1 Degrader-1 is a JNK1 PROTAC degrader with a DC50 of 10 nM. PROTAC JNK1 Degrader-1 reduces the level of fibronectin. PROTAC JNK1 Degrader-1 can be used for the research of pulmonary fibrosis .
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- HY-177948
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G Protein-coupled Receptor Kinase (GRK)
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Cardiovascular Disease
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GRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research .
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- HY-177744
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Molecular Glues
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Cancer
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GSPT2 degrader-1 (compound 619) is a selective molecular glue GSPT2 degrader targeting GSPT2. GSPT2 degrader-1 contains Thalidomide (HY-14658) and the linker of MDEG-541 (HY-150259). GSPT2 degrader-1 induces the degradation, but not GSPT1 or myelocytomatosis oncogene (MYC). GSPT2 degrader-1 can be used for research of gastrointestinal cancer .
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- HY-177791
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PROTACs
Influenza Virus
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Infection
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vRNPs degrader-1 is a potent PROTAC viral ribonucleoproteins (vRNPs) degrader. vRNPs degrader-1 shows broad-spectrum anti-influenza A viruses (IAV) activity by targeting the conserved 5′ end of viral RNA, thereby inducing proteasomal degradation of viral proteins. vRNPs degrader-1 inhibits H1N1, H9N2, and H3N2 infection in mice. vRNPs degrader-1 can be used for influenza research .
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- HY-144657
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PROTACs
Ras
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Cancer
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(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .
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- HY-176451
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CDK
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Cancer
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CDK9 degrader-1 (Compound AZ-9) is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model .
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- HY-134725
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- HY-173135
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PROTACs
Histone Demethylase
Apoptosis
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Cancer
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PROTAC KDM4 degrader-1 is a KDM4 PROTAC degrader that degrades KDM4A-C with DC50 values of 37.53, 39.93, and 49.41 nM, respectively, while sparing KDM4D. PROTAC KDM4 degrader-1 induces cell cycle arrest, apoptosis and antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 can be used for the research of esophageal cancer .
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- HY-173560
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ATTECs
SHP2
Apoptosis
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Cancer
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SHP2 ATTEC degrader-1 is a SHP2 ATTEC degrader. SHP2 ATTEC degrader-1 has degradation rate of 83.31 at 1.0 μM for 24 h in the PANC-1 cell line. SHP2 ATTEC degrader-1 inhibits cell growth in vivo and in vitro. SHP2 ATTEC degrader-1 induces apoptosis and increases the expression of the epithelial marker ( E-cadherin), and reduces the expression of interstitial markers (such as N-cadherin, Vimentin) (Pink: LC3 ligand (HY-174085); Black :linker HY-140468; Blue: SHP2 ligand (HY-174084) .
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- HY-128838A
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PROTACs
Estrogen Receptor/ERR
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Others
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(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader .
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- HY-162679
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c-Met/HGFR
Apoptosis
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Cancer
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|
c-Met degrader-1 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors .
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-
- HY-174856
-
|
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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))
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-
- HY-145071
-
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PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader .
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-
- HY-173369
-
|
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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) .
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-
- HY-156083
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors .
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-
- HY-147654
-
|
|
PROTACs
Influenza Virus
|
Infection
|
|
PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity .
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-
- HY-156244
-
|
|
PROTACs
|
Cancer
|
|
PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models .
|
-
- 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) .
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-
- HY-181598
-
|
|
HyT
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model .
|
-
- HY-186212
-
|
|
PROTACs
Survivin
PARP
|
Neurological Disease
Cancer
|
|
PROTAC survivin degrader-1 is an orally active, CNS-penetrant survivin-targeting PROTAC. PROTAC survivin degrader-1 induces degradation of survivin via the ubiquitin proteasome system. PROTAC survivin degrader-1 can be used for the research of glioblastoma .
|
-
- HY-179682
-
|
|
HDAC
NOD-like Receptor (NLR)
Interleukin Related
Caspase
|
Inflammation/Immunology
|
|
HDAC3 degrader-1 (Compound Z8) is a selective HDAC3 degrader with a DC50 of 2.42 μM. HDAC3 degrader-1 has almost no effect on HDAC1, HDAC2, and HDAC6. HDAC3 degrader-1 inhibits the activation of the NLRP3 inflammasome and reduces the secretion of IL-1β and caspase-1. HDAC3 degrader-1 shows significant efficacy in septic shock and colitis models. HDAC3 degrader-1 can be used in anti-inflammatory research .
|
-
- HY-181594
-
|
|
PROTACs
SNIPERs
YAP
|
Cancer
|
|
PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma .
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-
- HY-103628R
-
|
|
Reference Standards
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 Degrader-1 (Standard) is the analytical standard of PROTAC CDK9 Degrader-1 (HY-103628). This product is intended for research and analytical applications. PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
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-
- HY-181692
-
|
|
PROTACs
Epigenetic Reader Domain
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma .
|
-
- HY-183785
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Inflammation/Immunology
|
|
PROTAC ALK5 Degrader-1 is a selective ALK5 PROTAC degrader. PROTAC ALK5 Degrader-1 induces ALK5 degradation via ALK5 ATP-binding pocket engagement, CRBN recruitment, and the ubiquitin-proteasome system.PROTAC ALK5 Degrader-1 inhibits ALK5 downstream signaling. PROTAC ALK5 Degrader-1 can be used for the research of pulmonary fibrosis .
|
-
- HY-171441
-
|
|
STAT
|
Inflammation/Immunology
Cancer
|
|
STAT6 degrader-1 (Compound 21) is a bifunctional molecular glue degrader of STAT6 that recruits E3 ubiquitin ligase. STAT6 degrader-1 induces proteasomal degradation of STAT6. STAT6 degrader-1 is applicable to the research of cancer, inflammatory diseases and colorectal cancer .
|
-
- HY-185358
-
|
|
PROTACs
MALT1
|
Cancer
|
|
PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader. PROTAC MALT1 Degrader-1 is applicable to lymphoma research .
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-
- HY-171823
-
|
|
PROTACs
HMG-CoA Reductase (HMGCR)
|
Metabolic Disease
|
|
PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research .
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-
- HY-181653
-
|
|
PROTACs
E1/E2/E3 Enzyme
DNA/RNA Synthesis
JAK
STAT
Apoptosis
|
Cancer
|
|
PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research .
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-
- HY-181767
-
|
|
PROTACs
HDAC
Bcl-2 Family
Apoptosis
|
Cancer
|
|
PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia .
|
-
- HY-182775
-
-
- HY-181813
-
|
|
PROTACs
Ligands for E3 Ligase
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
PROTAC DHFR Degrader-1 is a selective PROTAC degrader targeting Plasmodium falciparum DHFR-TS with a Ki of 2.01 nM. PROTAC DHFR Degrader-1 exhibits no inhibitory activity against human DHFR and suppresses the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 can be used for the research of Plasmodium falciparum and malaria .
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-
- HY-103633R
-
|
|
Reference Standards
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BET Degrader-1 (Standard) is the analytical standard of PROTAC BET Degrader-1 (HY-103633). This product is intended for research and analytical applications. PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
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-
- HY-181705
-
|
|
PROTACs
Glycosidase
|
Metabolic Disease
|
|
PROTAC RTA Degrader-1 (Compound 3A) is a ricin toxin A chain (RTA) PROTAC degrader. PROTAC RTA Degrader-1 forms stable ternary complexes, maintains sustained hydrogen bonding interactions, and exhibits distinct interaction energy. PROTAC RTA Degrader-1 is applicable to research related to ricin toxin poisoning .
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-
- HY-181660
-
|
|
PROTACs
IKK
Apoptosis
|
Cancer
|
|
PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer .
|
-
- HY-181147
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia .
|
-
- HY-179321
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC4 Degrader-1 (compound SCT-1) is a potent and selective PROTAC HDAC4 degrader. PROTAC HDAC4 Degrader-1 reduces HDAC4 protein level, induces S phase cell cycle arrest, and inhibits cell colony formation, thereby inhibiting proliferation of the tumor cells. PROTAC HDAC4 Degrader-1 exhibits efficacy in a H460 mouse model. PROTAC HDAC4 Degrader-1 can be used for cancer research, such as lung cancer .
|
-
- HY-181879
-
|
|
PROTACs
Huntingtin
|
Neurological Disease
|
|
PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin (mHTT) PROTAC degrader. PROTAC mHTT Degrader-1 specifically recognizes pathogenic mHTT aggregates and recruits Cereblon (CRBN), thereby inducing ubiquitination and proteasomal degradation of mHTT. PROTAC mHTT Degrader-1 alleviates mHTT-induced cytotoxicity and neuroinflammation. In the R6/2 Huntington's disease mouse model, PROTAC mHTT Degrader-1 reduces cerebral protein aggregation levels and improves body weight, motor coordination and survival rate of animals. PROTAC mHTT Degrader-1 can be used for research on PROTAC therapies for Huntington's disease and other neurodegenerative diseases .
|
-
- HY-179467
-
|
|
PROTACs
Carbonic Anhydrase
|
Cancer
|
|
PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII .
|
-
- HY-181534
-
|
|
PROTACs
YAP
IAP
SNIPERs
|
Cancer
|
|
PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma .
|
-
- HY-181834
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML) .
|
-
- HY-181293
-
|
|
PROTACs
AAK1
|
Cancer
|
|
PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC50 of <10 nM. PROTAC AAK1 degrader-1 does not significantly impact the levels of any other NAK family members, including BMP2K, GAK, and STK16. PROTAC AAK1 degrader-1 can be used in ovarian cancer research .
|
-
- HY-181011
-
|
|
PROTACs
Phosphatase
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PROTAC Cdc25 degrader-1 (Compound D3) is an efficient Cdc25 PROTAC degrader. Its DC50 values for Cdc25A, Cdc25B, and Cdc25C are 0.97, 2.02, and 4.67 μM respectively. PROTAC Cdc25 degrader-1 induces cell cycle arrest and apoptosis in cancer cells and inhibits cell migration ability. PROTAC Cdc25 degrader-1 significantly increases the ROS level. PROTAC Cdc25 degrader-1 can be used for the study of colorectal adenocarcinoma .
|
-
- HY-182956
-
|
|
Molecular Glues
DNA Methyltransferase
|
Cancer
|
|
DNMT1 Degrader-1 is a selective DNMT1 degrader with an IC50 of 202.87 nM and a Kd value of 122 nM. As a molecular glue, DNMT1 Degrader-1 forms a ternary complex with DNMT1 and UHRF1, thereby triggering UHRF1-mediated ubiquitination and degradation of DNMT1, and inhibiting the enzymatic activity of DNMT1. DNMT1 Degrader-1 inhibits the proliferation of primary acute myeloid leukemia cells and exerts anti-tumor activity. DNMT1 Degrader-1 can be used for the research of acute myeloid leukemia .
|
-
- HY-181895
-
|
|
RET
|
Cancer
|
|
PROTAC HyTTD Degrader-1 (Compound B2) is a hydrophobic tag tethered degrader (HyTTD) targeting RET, as well as a degrader of the CCDC6-RET fusion protein. PROTAC HyTTD Degrader-1 induces the degradation of the CCDC6-RET fusion protein via the ubiquitin-proteasome pathway. PROTAC HyTTD Degrader-1 is applicable to the research of RET-driven cancers .
|
-
- HY-182796
-
|
|
HyT
JNK
|
Cancer
|
|
JNK1 degrader-1 is a JNK1 HyT degrader. JNK1 degrader-1 can induce JNK1 degradation through the HyT-mediated ubiquitin-proteasome system and autophagy-lysosome pathway. JNK1 degrader-1 inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT). JNK1 degrader-1 can be used for research on fibrotic diseases and cancer metastasis. (Pink: JNK1 ligand (HY-183006); Blue: Hyt hydrophobic group (HY-W037848); Black: Linker (HY-B1008)) .
|
-
- HY-183013
-
|
|
PROTACs
PARP
Apoptosis
|
Cancer
|
|
PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer .
|
-
- HY-180889
-
|
|
PROTACs
Epigenetic Reader Domain
|
Neurological Disease
Inflammation/Immunology
|
|
PROTAC BRD3 degrader-1 (compound D072) is a potent and selective PROTAC BRD3 degrader. PROTAC BRD3 degrader-1 selectively degrades BRD3 in mice, leading to the downregulation of H3K18ac without affecting BRD2 or BRD4. PROTAC BRD3 degrader-1 reduces intraocular inflammation in the experimental autoimmune uveitis (EAU) mouse mode and inhibits proinflammatory microglia in both uveitis retina and LPS (HY-D1056) treated mouse microglia cell line BV2. PROTAC BRD3 degrader-1 can be used for uveitis research .
|
-
- HY-103636R
-
|
|
Reference Standards
Sirtuin
PROTACs
|
Cancer
|
|
PROTAC Sirt2 Degrader-1 (Standard) is the analytical standard of PROTAC Sirt2 Degrader-1 (HY-103636). This product is intended for research and analytical applications. PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM) .
|
-
- HY-181695
-
|
|
PROTACs
Histone Acetyltransferase
|
Cancer
|
|
PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance .
|
-
- HY-168037A
-
|
|
PIN1
|
Cancer
|
|
PROTAC PIN1 degrader-1 TFA 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 .
|
-
- HY-182970
-
|
|
PROTACs
HIV
Interleukin Related
|
Inflammation/Immunology
|
|
PROTAC SAMHD1 Degrader-1 is an orally active targeted SAMHD1 PROTAC degrader, with an IC50 of 6.3 μM against the dNTP hydrolase activity of SAMHD1. PROTAC SAMHD1 Degrader-1 binds to SAMHD1 inside cells and mediates its degradation, with low off-target effects. PROTAC SAMHD1 Degrader-1 inhibits the production of pro-inflammatory cytokines and interferes with the cascade amplification process of inflammatory responses. PROTAC SAMHD1 Degrader-1 delays the progression of pulmonary fibrosis and exerts protective effects on lung tissues. PROTAC SAMHD1 Degrader-1 can be used in pulmonary fibrosis-related research. (Pink: SAMHD1 Target protein ligand (HY-182973); Blue: DCAF1 ligand (HY-182974); Black: linker (HY-W067705)) .
|
-
- HY-171801
-
|
|
PROTACs
LRRK2
|
Neurological Disease
|
|
PROTAC LRRK2 Degrader-1 (compound 18) is a leucine-rich repeat kinase 2 (LRRK2) PROTAC degrader with an IC 50 value less than 10 nM. PROTAC LRRK2 Degrader-1 can be used in the research of Parkinson's disease .
|
-
- HY-180177
-
|
|
PROTACs
|
Cancer
|
|
PROTAC BLIMP-1 degrader-1 (Compound 49) is a PROTAC-based BLIMP-1 degrader. PROTAC BLIMP-1 degrader-1 promotes the ubiquitination and degradation of BLIMP-1 and can be used in research on myeloproliferative tumors .
|
-
- HY-149845
-
|
|
PROTACs
GSK-3
|
Neurological Disease
|
|
PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease .
|
-
- HY-155816
-
|
|
PROTACs
|
Cancer
|
|
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
|
-
- HY-138536
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines .
|
-
- HY-175280
-
|
|
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) .
|
-
- HY-179688
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2/4 Degrader-1 (Compound 5) is a CDK2/4 PROTAC degrader, with its DC50 values for CDK2 and CDK4 both ≤ 10 nM. PROTAC CDK2/4 Degrader-1 exhibits excellent inhibitory activity against cell proliferation in OVCAR3 and T47D cells. PROTAC CDK2/4 Degrader-1 can be used for research on breast cancer and ovarian cancer .
|
-
- HY-148521
-
|
|
CDK
FLT3
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML .
|
-
- HY-147943
-
|
|
PROTACs
Btk
|
Cancer
|
|
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-150608
-
|
|
PROTACs
STING
|
Inflammation/Immunology
Cancer
|
|
PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC50 of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs). (Pink: STING ligand (HY-138682); Blue: CRBN ligand (HY-10984); Black: linker (HY-W015883)) .
|
-
- HY-179283
-
|
|
PROTACs
SARS-CoV
|
Infection
|
|
PROTAC SARS-CoV-2 RdRp Degrader-1 (PROTAC 10) is a SARS-CoV-2 RdRp PROTAC degrader, with a DC50 of 1.97 μM (in infected cells). PROTAC SARS-CoV-2 RdRp Degrader-1 promotes the ubiquitination and degradation of SARS-CoV-2 RdRp. PROTAC SARS-CoV-2 RdRp Degrader-1 can be used in the research of SARS-CoV-2 infection .
|
-
- HY-172208
-
|
|
PROTACs
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
PROTAC cGAS degrader-1 is a potent and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis .
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- HY-180907
-
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PROTACs
|
Cancer
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|
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 .
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-
- HY-176860
-
-
- HY-146324
-
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PROTACs
Apoptosis
CaMK
|
Cancer
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|
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 .
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- HY-181727
-
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Androgen Receptor
HSP
CDK
|
Cancer
|
|
AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .
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-
- HY-157764
-
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PROTACs
ATM/ATR
|
Cancer
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|
PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC50 of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research .
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-
- HY-130614
-
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PROTACs
Histone Methyltransferase
|
Cancer
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|
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 .
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-
- HY-175756
-
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Molecular Glues
SWI/SNF Complex
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Cancer
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|
SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4 DCAF16 and CRL1 FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer .
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-
- HY-179055
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PROTACs
DAPK
|
Neurological Disease
|
|
PROTAC DAPK1 Degrader-1 (Compound CP1) is a DAPK1 PROTAC degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increased the MDM2 protein level. PROTAC DAPK1 Degrader-1 significantly reduced the levels of cleaved caspase-3 and cleaved PARP in a cell apoptosis model induced by the neurotoxin ceramide, indicating that it effectively inhibits neuronal apoptosis by degrading DAPK1. PROTAC DAPK1 Degrader-1 can be used to study neurological diseases such as cerebral ischemia and traumatic brain injury (pink: DAPK1 ligand (HY-179071); blue: CRBN ligand (HY-10984); black: linker (HY-40171)) .
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-
- HY-168641
-
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PROTACs
Apoptosis
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC50 value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis. (Pink: ligand for target protein (HY-111387); black: linker (HY-W013731); Blue: E3 ligase ligand (HY-112078)) .
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-
- HY-177008
-
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PROTACs
EGFR
Apoptosis
Akt
ERK
|
Cancer
|
|
PROTAC HER2 degrader-1 is a highly selective HER2 PROTAC degrader, with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 induces apoptosis in BT-474 cells. PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573) .
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-
- HY-182275
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
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-
- HY-182958
-
|
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Hsp-targeting Chimeras
Epigenetic Reader Domain
HSP
|
Cancer
|
|
Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)) .
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-
- HY-133131
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression .
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-
- HY-153881
-
|
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Ras
|
Cancer
|
|
KRAS G12C degrader-1 (Compound 283) is a potent KRAS G12C degrader (DC50: < 100 nM) for cancer research. KRAS G12C degrader-1 is a chaperone (HSP90)-mediated protein degrader (CHAMPs) .
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-
- HY-168057
-
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PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC50 of 100-500 nM .
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-
- HY-179071
-
-
- HY-147656
-
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ATTECs
NAMPT
Autophagy
|
Cancer
|
|
NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency .
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-
- HY-145615
-
|
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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|
Pomalidomide-C12-NH2 hydrochloride is the E3 ligase ligand-linker conjugate of PROTAC KRAS G12C degrader-1 (HY-139186). PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS G12C degrader .
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-
- HY-181052
-
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PROTACs
Trk Receptor
|
Cancer
|
|
PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors .
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-
- HY-153880
-
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LYTACs
Ras
|
Cancer
|
|
KRAS degrader-1 is a potent KRAS degrader. KRAS degrader-1 targets specific proteins for degradation via the autophagy-lysosomal degradation pathway. KRAS degrader-1 is suitable for use in cancer research. (Blue: KRAS G12C-IN-72 (HY-128414); Black: Linker (HY-175587); Pink: 5-Iodoindolin-2-one (HY-76986); Blue + Black: KRAS ligand-Linker Conjugate 7 (HY-175586)) .
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-
- HY-181084
-
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PROTACs
BCL6
Aquaporin
PARP
Caspase
CDK
|
Cancer
|
|
PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader that targets BCL6 and GSPT1. PROTAC BCL6/GSPT1 Degrader-1 inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis in diffuse large B-cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 can be used for research on tumors such as lymphoma .
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-
- HY-170995
-
|
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PROTACs
ROR
Apoptosis
|
Cancer
|
|
PROTAC ROR1 degrader-1 is a ROR1 PROTAC degrader with DC50 values of 40.88 nM (NCI-H23), 69.0 nM (NCI-H460), 83.35 nM (NCI-H1299) and 42.07 nM (NCI-H1975), respectively. PROTAC ROR1 degrader-1 inhibits the proliferation of lung cancer cells and induces apoptosis. PROTAC ROR1 degrader-1 can be used in research related to non-small cell lung cancer .
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-
- HY-185634
-
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PROTACs
GSK-3
Tau Protein
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Neurological Disease
|
|
PROTAC GSK3 degrader-1 is a potent, blood-brain barrier-permeable GSK3 PROTAC degrader, with a DC50 of 1.4 nM against GSK3β. PROTAC GSK3 degrader-1 exerts equally potent degradation activity against both GSK3α and GSK3β. It inhibits the phosphorylation of CRMP2, PRKAA1 and Tau, and stabilizes β-catenin. PROTAC GSK3 degrader-1 can be used in the research of Alzheimer's disease and Parkinson's disease .
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-
- HY-171826
-
|
|
CDK
PROTACs
|
Cancer
|
|
PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research .
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-
- HY-162331
-
|
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Molecular Glues
STING
|
Inflammation/Immunology
Cancer
|
|
STING Degrader-1 (compound 2), a molecular glue, is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 exhibits a "hook effect", that degrades 75% STING protein at 10 μM, and degrades ca. 30% STING protein at 30 μM .
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-
- HY-155643
-
|
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PROTACs
Glutaminase
|
Cancer
|
|
PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a KD of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner .
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-
- HY-156591
-
|
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PROTACs
Mixed Lineage Kinase
Necroptosis
|
Others
|
|
PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC50 of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death .
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-
- 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 .
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-
- HY-139186
-
|
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PROTACs
Ras
|
Cancer
|
|
PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS G12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRAS G12C dimerization and degrades GFP- KRAS G12C in reporter cells .
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-
- HY-161749
-
|
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PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
PROTAC ALK degrader-1 (compound B1) is an ALK degrader based on PROTACs, with the DC50 of 26 nM in H3122 EML4-ALK. PROTAC ALK degrader-1 can be used to synthesis PROTAC ALK degrader-2 (HY-161750) with superior bioavailability .
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-
- HY-158985
-
|
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AUTACs
Autophagy
|
Cancer
|
|
Amino-PEG3-2G degrader-1 (compound ) is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 can be used to synthesize autophagy-targeting chimeras (AUTACs) .
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-
- HY-181568
-
|
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PROTACs
Aurora Kinase
DNA/RNA Synthesis
Apoptosis
|
Neurological Disease
Cancer
|
|
PROTAC Aurora A Degrader-1 (Compound 280) is a blood-brain barrier-permeable selective Aurora A PROTAC degrader, with DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively. PROTAC Aurora A Degrader-1 induces the formation of a ternary complex between AURKA and CRBN, degrades AURKA, reduces MYCN levels, induces DNA damage and apoptosis, exerts antiproliferative activity in cancer cells, and regulates the immune system. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer .
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-
- HY-163938
-
|
|
PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
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-
- HY-179077
-
|
|
PROTACs
Btk
IKZF Family
|
Cancer
|
|
PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma . (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))
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-
- HY-168593
-
|
|
β-catenin
PROTACs
Wnt
Histone Demethylase
|
Cancer
|
|
PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547) .
|
-
- HY-175370
-
|
|
PROTACs
RIP kinase
|
Cancer
|
|
PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373) .
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-
- HY-186132
-
|
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PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer) .
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-
- 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))
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-
- HY-181536
-
|
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Ligands for Target Protein for PROTAC
YAP
|
Cancer
|
|
TEAD ligand 2 is a target protein ligand that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-1 (HY-181534). PROTAC TEAD1/IAP degrader-1 is a potent TEAD1/IAP PROTAC degrader with anti-cancer activity .
|
-
- HY-176875
-
|
|
Molecular Glues
|
Cancer
|
|
CoREST/LSD1 degrader-1 (Compound 4) is a molecular glue degrader targeting the KBTBD4 E3 ubiquitin ligase. CoREST/LSD1 degrader-1 is promising for research of KBTBD4-mutant driven cancers (e.g., medulloblastoma) and epigenetic dysregulation disorders .
|
-
- HY-178034
-
|
|
PROTACs
Oxysterol-binding Protein-related Protein (ORP)
|
Cancer
|
|
PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells . Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
|
-
- HY-130709
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .
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-
- HY-182297
-
-
- HY-179064
-
|
|
Target Protein Ligand-Linker Conjugates
IKZF Family
|
Cancer
|
|
IKZF1/3 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC IKZF1/3 Degrader-1 (HY-179075). PROTAC IKZF1/3 Degrader-1 is a potent IKZF1/3 PROTAC degrader with neuroprotective activity .
|
-
- HY-180428
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRM/BRG1 ATP degrader-1 (Compound 1) is a BRG1/BRM degrader with IC50 values for the degradation of BRM IF and BRG1 IF of 0.01-0.1 μM and > 0.1 μM respectively. BRM/BRG1 ATP degrader-1 can be used for cancer research .
|
-
- HY-103628
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
|
-
- HY-182971
-
|
|
PROTACs
Enterovirus
|
Infection
|
|
PROTAC EV-A71 Degrader-1 is a PROTAC degrader targeting EV-A71 3D polymerase, with broad-spectrum activity against a variety of enteroviruses. PROTAC EV-A71 Degrader-1 induces the degradation of EV-A71 3D polymerase through the ubiquitin-proteasome and autophagy-lysosome pathways, and blocks viral replication. PROTAC EV-A71 Degrader-1 protects infected mice from death, alleviates tissue damage, and exhibits safety profiles. PROTAC EV-A71 Degrader-1 can be used in the research of enterovirus infections. (Pink: EV-A71 ligand (HY-19339); Blue: E3 ligase ligand (HY-W012479); Black: linker (HY-W105744)) .
|
-
- HY-182083
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer .
|
-
- HY-176428
-
|
P11-2
|
PROTACs
MNK
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
|
-
- HY-174405
-
|
|
PROTACs
Phosphodiesterase (PDE)
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model . Pink: PDE4 ligand (HY-174410); Blue: CRBN ligase ligand (HY-10984); Black: linker
|
-
- HY-170669
-
|
|
PROTACs
CRM1
Apoptosis
NF-κB
|
Cancer
|
|
PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)) .
|
-
- HY-155008
-
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PROTACs
Hexokinase
|
Cancer
|
|
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
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-
- HY-145479
-
|
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PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC50 of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))
|
-
- HY-163757
-
|
|
PROTACs
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) .
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-
- HY-133138
-
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) . PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
|
-
- HY-125877
-
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|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .
|
-
- HY-161110
-
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Amyloid-β
|
Neurological Disease
|
|
APP degrader-1 (Compound 0152) is an orally active amyloid precursor protein (APP) degrader that induces APP degradation and reduces the extracellular release of Aβ42. APP degrader-1 can bind to both CAPRIN1 and APP, and enhances their interaction as well as CAPRIN1-mediated APP degradation through the endosome-lysosome pathway .
|
-
- HY-179066
-
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 212 is a PROTAC E3 ligase-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC IKZF1/3 Degrader-1 (HY-179075). PROTAC IKZF1/3 Degrader-1 is a potent IKZF1/3 PROTAC degrader with neuroprotective activity .
|
-
- HY-149678
-
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PROTACs
|
Cancer
|
|
PROTAC eDHFR Degrader-1 is a PROTAC that is effective degradation of eDHFR-YFP, various POIs-including YFP and Luciferase .
|
-
- HY-130499
-
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Target Protein Ligand-Linker Conjugates
|
Cancer
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|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader .
|
-
- HY-163851
-
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|
PROTACs
HIV
|
Infection
|
|
PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC50: 33.35 μM against HIV-1IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852) .
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-
- HY-163440
-
|
|
PROTACs
NAMPT
|
Cancer
|
|
PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells.
(Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
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-
- HY-143904
-
|
|
PROTACs
Mps1
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-112100
-
|
|
PROTAC-Linker Conjugates for PAC
Estrogen Receptor/ERR
|
Cancer
|
|
MC-Val-Cit-PAB-PROTAC ERα Degrader-1 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. MC-Val-Cit-PAB-PROTAC ERα Degrader-1 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
|
-
- HY-115865
-
|
|
IAP
|
Cancer
|
|
XIAP degrader-1, a primary amine tethered small molecule, promotes the degradation of X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-178695
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Infection
|
|
E3 Ligase Ligand-linker Conjugate 216 is a conjugate of an E3 ligase CRBN ligand and a linker. E3 Ligase Ligand-linker Conjugate 216 can be used to synthesize PROTAC SARS-CoV-2 RdRp Degrader-1 (HY-179283). PROTAC SARS-CoV-2 RdRp Degrader-1 is a SARS-CoV-2 RdRp PROTAC degrader .
|
-
- HY-130612
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-111844
-
|
|
PROTACs
SNIPERs
RAR/RXR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .
|
-
- HY-163609
-
|
|
PROTACs
Aldose Reductase
|
Cancer
|
|
PROTAC AKR1C3 degrader-1 (compound 5) is a potent AKR1C3 PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .
|
-
- HY-148837
-
|
|
PROTACs
c-Myc
Casein Kinase
|
Infection
Cardiovascular Disease
Cancer
|
|
PROTAC c-Myc degrader-1 (Compound A153) is a multiple target protein degrader (PROTAC). PROTAC c-Myc degrader-1 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. PROTAC c-Myc degrader-1 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection (Pink: c-Myc ligand (HY-168685); Blue: E3 ligase ligand (HY-W093472); Black: linker (HY-W015808)) .
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-
- HY-181758
-
|
|
PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
c-Myc
Apoptosis
|
Cancer
|
|
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
|
-
- HY-176239
-
|
|
PROTACs
PI3K
Akt
Apoptosis
Autophagy
|
Cancer
|
|
PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
|
-
- HY-157763
-
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PROTAC-Linker Conjugates for PAC
Btk
|
Cancer
|
|
Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding BTK bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces BTK degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo BTK degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)) .
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-
- HY-179715
-
|
|
PROTACs
JAK
TNF Receptor
Interleukin Related
STAT
|
Inflammation/Immunology
|
|
PROTAC JAK1/2 degrader-1 (Compound A8) is a selective JAK1/2 PROTAC degrader, with DC50 values of 1.4 μM for JAK1 and 0.92 μM for JAK2. PROTAC JAK1/2 degrader-1 significantly inhibits the release of NO, IL-6 (IC50 = 12.89 μM) and TNF-α (IC50 = 17.17 μM). PROTAC JAK1/2 degrader-1 significantly alleviates inflammatory responses and colonic damage by inhibiting the JAK/STAT3 signaling pathway. PROTAC JAK1/2 degrader-1 can be used for research on colitis. (Pink: JAK1/2 ligand (HY-179716); Blue: CRBN ligand (HY-10984); Black: linker; CRBN ligand + linker (HY-131888A)) .
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-
- HY-181153
-
|
|
PROTACs
FGFR
|
Cancer
|
|
PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma .
|
-
- HY-131188
-
|
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PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively .
|
-
- HY-130620
-
|
|
PROTAC Linkers
|
Cancer
|
|
PEG3-C4-OBn is a polyethylene glycol (PEG)-based PROTAC linker. PEG3-C4-OBn can be used in the synthesis of the PROTAC SGK3 degrader-1 (HY-125878). PROTAC SGK3 degrader-1 is a potent SKG3 degrader based on PROTAC .
|
-
- HY-169008
-
|
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PROTACs
Acetyl-CoA Carboxylase
|
Infection
|
|
PROTAC ACC degrader-1 (Compound 9b) is a Acetyl-CoA Carboxylase degrader. PROTAC ACC degrader-1 exhibits superior potency against Aphis craccivora (IC50 = 107.8 μg/mL). (Structure Note: Pink, Target protein ligand (HY-169009); Blue, E3 ligand (HY-10984); Black, linker (HY-W007559) .
|
-
- HY-175373
-
|
|
PROTAC Linkers
|
Others
|
|
Bispiperidin-piperazin-acetate is a PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC RIPK1 Degrader-1 (HY-175370) .
|
-
- HY-185575
-
-
- HY-111840
-
|
|
SNIPERs
PROTACs
|
Cancer
|
|
PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand .
|
-
- HY-128840
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
PROTAC MDM2 Degrader-1 (Compound 15a) is a MDM2 PROTAC degrader. The structures of both Linker ends of PROTAC MDM2 Degrader-1 are MDM2 ligands. PROTAC MDM2 Degrader-1 can not only block the binding of p53-MDM2, but also degrade the target MDM2 protein by utilizing the function of the E3 ligase of MDM2 itself, thus exerting an anti-tumor effect. (Pink: MDM2 ligand 2 (HY-128836); Black: Linker (HY-128844); Blue: E3 ligase Ligand 15 (HY-128836))
|
-
- HY-151110
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-178858
-
|
|
PROTACs
FLT3
Checkpoint Kinase (Chk)
STAT
ERK
c-Myc
Akt
|
Cancer
|
|
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .
|
-
- HY-168276
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-Nonanol is a PROTAC linker. Boc-Nonanol can be used in the synthesis of PROTAC TRIB2 degrader-1 (HY-168274) .
|
-
- HY-176489
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc . Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
|
-
- HY-151110A
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-163920
-
|
|
PROTACs
HDAC
|
Cancer
|
|
Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells .
|
-
- HY-162412
-
|
|
PROTACs
Adrenergic Receptor
Apoptosis
|
Cancer
|
PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .
|
-
- HY-W998238
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-5-F-6-azetidin-MeOH is a synthesized E3 ligase ligand-linker conjugate that can be used for synthesis of PROTAC FLT3/CHK1 Degrader-1 (HY-178858). PROTAC FLT3/CHK1 Degrader-1 is a potent FLT3/CHK1 degrader with anti-tumor activity .
|
-
- HY-179076
-
|
|
Ligands for Target Protein for PROTAC
Btk
IKZF Family
|
Cancer
|
|
BTK/IKZF1/3 ligand 1 is a BTK/IKZF1/3 PROTAC ligand. BTK/IKZF1/3 ligand 1 can be conjugated with E3 ligase Ligand (HY-41547) and linker to synthesize PROTAC BTK/IKZF1/3 Degrader-1 (HY-179077). PROTAC BTK/IKZF1/3 Degrader-1 can be used for cancer research .
|
-
- HY-131911
-
|
|
PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
|
Inflammation/Immunology
|
|
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells .
|
-
- HY-129966
-
|
|
PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon-based IRAK4 PROTAC. PROTAC IRAK4 degrader-1 is composed of IRAK4 ligand (red part) PROTAC IRAK4 ligand-1 (HY-129967), E3 ligase ligand (blue part) Pomalidomide (HY-10984), and PROTAC linker (black part) AM-Imidazole-PA-Boc (HY-129968) .
|
-
- HY-178869
-
-
- HY-158400
-
-
- HY-103633
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
|
-
- HY-175653
-
-
- HY-181707
-
-
- HY-W007587
-
|
|
PROTAC Linkers
|
Cancer
|
|
9-Bromononanoic acid is a PROTAC linker. 9-Bromononanoic acid can be used in synthesis PROTAC FGFR1 degrader-1 (HY-170869) .
|
-
- HY-182973
-
-
- HY-W411604
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl hex-5-ynoate is the linker that can be used for PROTAC synthesis of PROTAC cGAS degrader-1 (HY-172208) .
|
-
- HY-170996
-
-
- HY-168191
-
-
- HY-134497
-
|
Rimonabat acomplia
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Rimonabant carboxylic acid is a Ligand for Target Protein for PROTAC. Rimonabant carboxylic acid can be used to synthesize PROTAC CB1R Degrader-1 (HY-178176) .
|
-
- HY-160262
-
-
- HY-180901
-
-
- HY-176186
-
|
|
PROTAC Linkers
|
Cancer
|
|
4-Hydroxy-1-piperidinepropanamide is a PROTAC linker that can be used in the synthesis of PROTAC DDR1 degrader-1 (HY-176184) .
|
-
- HY-W013381
-
|
Decanoic acid, 10-bromo-
|
PROTAC Linkers
|
Others
|
|
10-Bromodecanoic acid (Decanoic acid, 10-bromo-) is a linker that can be used in the synthesis of PROTACs, such as PROTAC KDM4 degrader-1 (HY-173135) .
|
-
- HY-176795
-
-
- HY-163152
-
-
- HY-183006
-
-
- HY-129968
-
|
|
PROTAC Linkers
|
Cancer
|
|
AM-Imidazole-PA-Boc is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966) .
|
-
- HY-175610
-
|
|
PROTACs
FLT3
JAK
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
|
-
- HY-178176
-
|
|
PROTACs
Cannabinoid Receptor
Akt
ERK
Bcl-2 Family
Apoptosis
|
Cancer
|
|
PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .
|
-
- HY-179112
-
|
|
PROTACs
IKK
Nuclear Hormone Receptor 4A/NR4A
Caspase
Necroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577) .
|
-
- HY-131183
-
|
|
PROTACs
PD-1/PD-L1
|
Inflammation/Immunology
|
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
|
-
- HY-130713
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .
|
-
- HY-168242
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRM/BRG1 degrader-1 (Example 253) is a PROTAC BRM/BRG1 degrader, with DC50 of 10-100 nM for BRM, > 1 μM for BRG1. PROTAC BRM/BRG1 degrader-1 can be used for cancer research. Blue: E3 ligase ligand (HY-168243), black: linker (HY-168244). Red: BRM/BRG1 inhibitor (HY-W539427) .
|
-
- HY-103636
-
|
|
Sirtuin
PROTACs
|
Cancer
|
|
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM) .
|
-
- HY-149236
-
-
- HY-174857
-
-
- HY-W584512
-
-
- HY-130819
-
|
|
PROTAC Linkers
|
Cancer
|
|
Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .
|
-
- HY-W041652
-
|
|
ADC Linker
|
Cancer
|
|
5-Hydroxypentanoic acid is a PROTAC linker. 5-Hydroxypentanoic acid can be used in the synthesis of PROTAC AR-V7 degrader-1 (HY-145479) .
|
-
- HY-168193
-
|
|
PROTAC Linkers
|
Cancer
|
|
5-Amino-N-(3-bromopropyl)pentanamide is a PROTAC linker used in the synthesis of PROTAC TBL1X degrader-1 (HY-168190) .
|
-
- HY-W442085
-
|
|
PROTAC Linkers
|
Cancer
|
|
1,4-Di(3-hydroxypropoxy)butane is the linker of PROTAC Aster-A degrader-1 (HY-D233) and can be used for the synthesis of PROTAC .
|
-
- HY-130621
-
|
|
PROTAC Linkers
|
Cancer
|
|
OTs-C6-OBn is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC SGK3 degrader-1 (HY-125878) .
|
-
- HY-168017
-
-
- HY-168695
-
-
- HY-W883326
-
|
|
Ligands for E3 Ligase
|
Others
|
|
CRBN ligand-902 is a CRBN E3 ligase ligand that can be used for synthesis of PROTAC CDK2/4 Degrader-1 (HY-179688) .
|
-
- HY-176490
-
-
- HY-130814
-
|
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .
|
-
- HY-W973851
-
-
- HY-176187
-
-
- HY-130852
-
-
- HY-168243
-
-
- HY-157804
-
|
|
PROTACs
SARS-CoV
|
Infection
|
|
PROTAC SARS-CoV-2 Mpro degrader-1 (compound 5) is a PROTAC degrader targeting the major SARS-CoV-2 protease with broad-spectrum antiviral activity .
|
-
- HY-172218
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Lenalidomide-hex-5-ynoic acid is a conjugate of E3 ligase ligand and linker, and can be used to synthesize PROTACs, such as PROTAC cGAS degrader-1 (HY-172208) .
|
-
- HY-176491
-
|
|
PROTAC Linkers
|
|
|
Alkyne-pyrazine-O-piperidine-(1-methylcyclopropyl) methanol is a PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC pan-KRAS degrader-1 (HY-176489) .
|
-
- HY-179075
-
|
|
PROTACs
BCL6
IKZF Family
|
Cancer
|
|
PROTAC BCL6/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BCL6/IKZF1/3 Degrader-1 exhibits superior antiproliferative effects in various germinal center B-cell-like (GCB) and activated B-cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cell lines. PROTAC BCL6/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma . (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179064); Blue: CRBN ligand (HY-41547); Black: linker (HY-42427); CRBN ligand-Linker: (HY-179066))
|
-
- 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))
|
-
- HY-176429
-
-
- HY-170672
-
-
- HY-43191
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 6-bromohexanoate is a PROTAC linker. tert-Butyl 6-bromohexanoate can be used to design PROTAC, such as PROTAC ERK5 degrader-1 (HY-176528) .
|
-
- HY-W539427
-
-
- HY-168277
-
-
- HY-186213
-
-
- HY-175359
-
-
- HY-173137
-
-
- HY-W1008330
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 197 is an E3 ubiquitinase ligand-linker conjugate that can be used to synthesize the PROTAC Androgen receptor degrader-1 (HY-175652) .
|
-
- HY-W087383
-
|
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide 5-fluoride is a thalidomide-based Cereblon ligand used to recruit Cereblon protein. Thalidomide 5-fluoride can be linked to target protein ligands (e.g. IRAK4) through a linker to form PROTAC molecules (e.g. PROTAC IRAK4 degrader-1). PROTAC IRAK4 degrader-1 caused <20%, >20-50%, and >50% IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, respectively .
|
-
- HY-175678
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD2 BD1 Degrader-1 (compound 21-1) is a potent and selective BRD2 BD1 PROTAC degrader. PROTAC BRD2 BD1 Degrader-1 induces the association of BRD2 BD1 and von Hippel–Lindau-elongin C-elongin B (VCB). (Pink: BRD2-BD1 Ligand (HY-175679); Blue: E3 ligase ligand (HY-125845); Black: Linker (HY-W069332)) .
|
-
- HY-168274
-
|
|
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .
|
-
- HY-138678B
-
-
- HY-185635
-
-
- HY-158678
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 27 (part of 15) is a ligand for E3 ligase, used for the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551)
|
-
- HY-178035
-
-
- HY-182975
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
E3 Ligase Ligand-linker Conjugate 229 is a conjugate of an E3 ligase ligand and a linker, which can be used for the synthesis of PROTAC SAMHD1 Degrader-1 (HY-182970) .
|
-
- HY-30105
-
|
|
PROTAC Linkers
|
Cancer
|
|
N-Boc-piperazine is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) .
|
-
- HY-176789
-
-
- HY-181535
-
-
- HY-169152
-
|
|
Ligands for E3 Ligase
|
Others
|
|
DCAF1 ligand 1 is a DCAF1 ligand, which can be used for the synthesis of PROTACs, such as PROTAC BRD4-DCAF1 degrader-1 (HY-169152) .
|
-
- HY-180902
-
-
- HY-137487
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells . (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.
|
-
- HY-173370
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
MAGL Ligand-Linker Conjugate 1 is a conjugate of the MAGL ligand and the linker. MAGL Ligand-Linker Conjugate 1 can be used for synthesis of PROTAC degrader PROTAC MAGL degrader-1 (HY-173369) .
|
-
- HY-181148
-
-
- HY-168018
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Demethyl-NSC682769 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Demethyl-NSC682769 can be used in synthesis PROTAC YAP degrader-1 (HY-168016) .
|
-
- HY-182974
-
|
|
Ligands for E3 Ligase
|
Others
|
|
DCAF1 binder 3 is a DCAF1 binder and an E3 ligase ligand. DCAF1 binder 3 can be used to synthesize PROTAC SAMHD1 Degrader-1 (HY-182970) .
|
-
- HY-169151
-
-
- HY-103632
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology .
|
-
- HY-156401
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader . BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062). (Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695) .
|
-
- HY-130816
-
|
VH032-O-Ph-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02 .
|
-
- HY-158679
-
-
- HY-168245
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 126 is an E3 Ligase Ligand-linker Conjugate, and can be used for synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-1 (HY-168242) .
|
-
- HY-176185
-
-
- HY-175654
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
6-(2,4-Dioxopyrimidin-1-yl)-1-methylindole is an E3 ligase ligand used in the synthesis of the PROTAC Androgen receptor degrader-1 (HY-175652) .
|
-
- HY-W004701
-
|
|
PROTAC Linkers
|
Cancer
|
|
Br-C3-methyl ester is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) .
|
-
- HY-175371
-
-
- HY-W940885
-
-
- HY-130821
-
|
|
PROTAC Linkers
|
Cancer
|
|
THP-PEG4-Pyrrolidine(N-Me)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .
|
-
- HY-130820
-
|
|
PROTAC Linkers
|
Cancer
|
|
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .
|
-
- HY-168275
-
-
- HY-174798
-
-
- HY-170671
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 49 serves as the E3 ubiquitin ligase ligand for PROTAC XPO1 degrader-1 (HY-170669). E3 ligase Ligand 49 can be utilized for the synthesis of PROTACs .
|
-
- HY-146393
-
|
|
PROTACs
Cytochrome P450
|
Cancer
|
|
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
|
-
- HY-183017
-
|
|
Target Protein Ligand-Linker Conjugates
|
Others
|
|
N-Descyclopropanecarbaldehyde olaparib-CO-C9-NHBoc (Compound 6h) is a target protein ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC PARP2 degrader-1 (HY-183013) .
|
-
- HY-176381
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
BTK ligand 11-alcohol-PEG6-azido is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as TDP-43 degrader-1 (HY-122828) .
|
-
- HY-168039
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-NH-Piperidine-C5-OH is a PROTAC linker. Boc-NH-Piperidine-C5-OH can be used in the synthesis of PROTAC PIN1 degrader-1 (HY-168037) .
|
-
- HY-168038
-
-
- HY-175680
-
-
- HY-159619
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-azetidine-2C-oxotetrahydropyrimidin-bromophenyl is a PROTAC Linker. Boc-azetidine-2C-oxotetrahydropyrimidin-bromophenyl can be used in the synthesis of PROTAC GSPT1 degrader-1 (HY-159609) .
|
-
- HY-176529
-
|
|
Ligands for Target Protein for PROTAC
ERK
|
Cancer
|
|
ERK5 ligand-1 is a is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). ERK5 ligand-1 can be used to design PROTAC, such as PROTAC ERK5 degrader-1 (HY-176528) .
|
-
- HY-181531
-
|
|
Ligands for E3 Ligase
IAP
|
Cancer
|
|
IAP ligand 7 is an E3 ligase ligand. IAP ligand 7 can be conjugated with TEAD ligand (HY-181595) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
|
-
- HY-163852
-
-
- HY-158677
-
|
|
Bcl-2 Family
|
Cancer
|
|
BcI-2/BcI-xI ligand 1 is a BcI-2/BcI-xI ligand, and can be used for synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551) .
|
-
- HY-112078B
-
|
|
Ligands for E3 Ligase
|
Others
|
|
(S,S,S)-AHPC-Me is an E3 ligase ligand. (S,S,S)-AHPC-Me can be used for synthesis of PROTAC (4S)-PROTAC SOS1 degrader-1 diTFA (HY-144657A) .
|
-
- HY-175679
-
-
- HY-182976
-
-
- HY-168192
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-amide-C3-Br is a conjugate of the E3 ligase ligand Thalidomide with a linker and can be used in the synthesis of PROTAC TBL1X degrader-1 (HY-168190) .
|
-
- HY-172370
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-Boc is the conjugate composed of an E3 ligase (Cereblon) ligand and a linker that can be used for synthesis of PROTAC CARM1/IKZF3 degrader-1 (HY-172368) .
|
-
- HY-175440
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-S-C6-acid is a synthetic E3 ligase ligand -linker conjugate, consisting of a thalidomide-based cereblon ligand and one linker. It can be used to synthesize PROTAC Cas9 Degrader-1 (HY-172113) .
|
-
- HY-172369
-
-
- HY-W013021
-
|
|
Ligands for E3 Ligase
|
Others
|
|
Norbornene is a cycloolefin and building block for synthesis of porous organic polymeric materials via metathesis, addition, and CANAL polymerization. Norbornene can also be used as an E3 ligase ligand for the synthesis of PROTAC, such as PROTAC HyTTD Degrader-1 (HY-181895) .
|
-
- HY-168244
-
|
|
PROTAC Linkers
|
Cancer
|
|
TsO-C2-Piperidine-O-azetidine-CO-Ph-C2-OH is a PROTAC linker, and can be used for PROTAC synthesis, such as PROTAC BRM/BRG1 degrader-1 (HY-168242) .
|
-
- HY-163960
-
|
|
PROTAC Linkers
|
Cancer
|
|
NH2-Ph-NH-cyclohexane-NH-Boc is a PROTAC linker. NH2-Ph-NH-cyclohexane-NH-Boc can be used in synthesis PROTAC erf3a Degrader-1 (HY-163938) .
|
-
- HY-178197
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 210 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 210 can be used to synthesize PROTAC CB1R Degrader-1 (HY-178176) .
|
-
- HY-180906
-
-
- HY-147525
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .
|
-
- HY-170673
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 156 is a CRBN E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 156 can be used to synthesize PROTAC XPO1 degrader-1 (HY-170669) .
|
-
- HY-125878
-
|
SGK3-PROTAC1
|
PROTACs
SGK
|
Cancer
|
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), a chemical probe, is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate) .
|
-
- HY-21999
-
|
Tert-butyl 6-aminohexanoate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 6-aminocaproate (Tert-butyl 6-aminohexanoate) is a PROTAC linker. tert-Butyl 6-aminocaproate can be used in synthesis PROTAC CARM1/IKZF3 degrader-1 (HY-172368) .
|
-
- HY-163864
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2 degrader-1 (compound I-321) is a PROTAC degrader of SMARCA with DC50<100nM (red: SMARCA inhibitor, black: linker (HY-Y1215), blue: E3 ligase ligand (HY-163927) ) .
|
-
- HY-169371
-
|
|
SOS1
Drug Intermediate
|
Others
|
|
SOS1 Ligand intermediate-7 (65) is an intermediate for the synthesis of SOS1 ligand (HY-111671). SOS1 activator 1 (HY-111671) can be used for the synthesis of PROTAC SOS1 degrader-1 (HY-145737) .
|
-
- HY-174461
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
|
-
- HY-181595
-
|
|
Ligands for Target Protein for PROTAC
YAP
|
Cancer
|
|
TEAD ligand 5 (Compound S19) is a TEAD PROTAC ligand. TEAD ligand 5 can be conjugated with E3 ligase Ligand (HY-181531) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
|
-
- HY-129967
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966) .
|
-
- HY-178198
-
|
|
PROTAC Linkers
|
Cancer
|
|
2-[4-(Aminomethyl)triazol-1-yl]ethanamine is a PROTAC Linker. 2-[4-(Aminomethyl)triazol-1-yl]ethanamine can be used to synthesize PROTAC CB1R Degrader-1 (HY-178176) .
|
-
- 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) .
|
-
- HY-174410
-
-
- HY-W1047040
-
-
- HY-168040
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C5-piperidine-NH-Boc is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-O-C5-piperidine-NH-Boc can be used to synthesize PROTAC PIN1 degrader-1 (HY-168037) .
|
-
- HY-168643
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Me-(S,R,S)-AHPC-PEG2-OTs is a conjugate of E3 ligase ligand and linker (E3 Ligase Ligand-Linker Conjugates) used in the synthesis of PROTAC HIF-1α degrader-1 (HY-168641) .
|
-
- HY-76986
-
|
5-iodo-2,3-dihydro-1H-indol-2-one
|
Drug Intermediate
|
Others
|
|
5-Iodoindolin-2-one (5-iodo-2,3-dihydro-1H-indol-2-one) is an intermediate that can be used in the synthesis of degraders, such as KRAS degrader-1 (HY-153880) .
|
-
- HY-W1115186
-
|
|
Ligands for E3 Ligase
|
Others
|
|
CRBN ligand-900 is an E3 ligase ligand that can be used in the recruitment of CRBN protein. CRBN ligand-900 can be connected to the NTRK1 ligand (HY-185545) by a linker to synthesis of PROTAC NTRK1 degrader-1 (HY-181052) .
|
-
- HY-131190
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
N-Boc-SBP-0636457-OH is a synthesized E3 ligase ligand-linker conjugate that incorporates IAP ligand and a linker. N-Boc-SBP-0636457-OH can be used to design a PROTAC Bcl-xL degrader-1 (HY-131188) .
|
-
- HY-180180
-
|
|
PROTAC Linkers
|
Cancer
|
|
trans-5-(4-(Hydroxymethyl)cyclohexyl)-6-methylpicolinic acid is a PROTAC linker. trans-5-(4-(Hydroxymethyl)cyclohexyl)-6-methylpicolinic acid can be used to synthesize PROTAC BLIMP-1 degrader-1 (HY-180177) .
|
-
- HY-168318
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Bestatin-amide-PEG3-CH2-acid is an E3 ligase ligand-linker conjugate. Bestatin-amide-PEG3-CH2-acid can be used to synthesize PROTAC RAR Degrader-1 (HY-111844) .
|
-
- 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) .
|
-
- HY-176430
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-amide-pimelic acid is an E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based CRBN ligand and Linker (HY-Y1139). Lenalidomide-amide-pimelic acid can be used for synthesis of PROTAC MNK1 degrader-1 (HY-176428) .
|
-
- HY-W1137162
-
|
|
Ligands for E3 Ligase
|
Others
|
|
CRBN ligand-904 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), which is used to recruit cereblon protein. CRBN ligand-904 can be linked to a target protein ligand via a linker to form a PROTAC, such as PROTAC GSK3 degrader-1 (HY-185634) .
|
-
- HY-159620
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide 5-azetidine-2C-oxotetrahydropyrimidin-bromophenyl is an E3 Ligase Ligand-Linker Conjugate. Thalidomide 5-azetidine-2C-oxotetrahydropyrimidin-bromophenyl can be used to synthesize PROTAC GSPT1 degrader-1 (HY-159609) .
|
-
- HY-41547
-
|
Cereblon ligand 4; E3 ligase Ligand 4
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966) .
|
-
- HY-178046
-
-
- HY-159777
-
-
- HY-130813
-
-
- HY-131189
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
N-Boc-SBP-0636457-OH, a ligand for E3 ubiquitin ligase, is used in the recruitment of IAP E3 ligases. N-Boc-SBP-0636457-OH can be connected to the ligand for Bcl-xL by a linker to form PROTAC Bcl-xL degrader-1 (HY-131188).
|
-
- HY-181897
-
|
|
Huntingtin
Ligands for Target Protein for PROTAC
|
Neurological Disease
|
|
mHTT ligand-1 is an mHTT ligand. As a Ligand for Target Protein for PROTAC, mHTT ligand-1 can be used to develop and design PROTAC-based mHTT degraders, such as PROTAC mHTT Degrader-1 (HY-181879). mHTT ligand-1 is applicable to research related to Huntington's disease .
|
-
- HY-131186
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C3-piperazine-N-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) .
|
-
- HY-176188
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-5-Br-amide-C2-Br is an E3 ligase ligand-linker conjugate. Lenalidomide-5-Br-amide-C2-Br can be used to synthesize PROTAC DDR1 degrader-1 (HY-176184) .
|
-
- HY-163904
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,R)-VH032-CO-C3-CONH-C2-PEG3-OH is an E3 ligase ligand-linker conjugate of PROTAC NCOA4 degrader-1 (HY-163897), which can be used for the synthesis of PROTACs .
|
-
- HY-182979
-
|
|
HSP
|
Cancer
|
|
HSP70 ligand 2 is an HSP70 ligand and serves as a ligand for PROTAC target proteins. HSP70 ligand 2 can be used to synthesize Hsp70TAC BRD4 Degrader-1 (HY-182958) and Hsp70TAC PD-1 Degrader-2 (HY-182959) .
|
-
- HY-158343
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-CH2 is a conjugate of E3 ligase ligand and linker. Thalidomide-NH-PEG2-C2-CH2 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .
|
-
- HY-175444
-
|
|
E3 Ligase Ligand-Linker Conjugates
IAP
|
Cancer
|
|
XIAP ligand-Linker Conjugate 1 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 (HY-175348) and linker. XIAP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098) .
|
-
- HY-185546
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
CRBN ligand-900 Gly is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugate) that incorporates a CRBN ligand and a linker. CRBN ligand-900 Gly can be connected to the target protein ligand to form a PROTAC NTRK1 degrader-1 (HY-181052) .
|
-
- HY-131184
-
|
|
PROTAC Linkers
|
Inflammation/Immunology
|
|
N-Boc-piperazine-C3-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-N-piperazine-C3-COOH can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183) .
|
-
- HY-168019
-
-
- HY-153606
-
|
|
Drug Derivative
HDAC
|
Cancer
|
|
VUBI1 analogue-1 (compound 79) is a VUBI1 (HY-111671) analogue. VUBI1 (SOS1 activator 1) is a SOS1 activator with a Kd of 44 nM. VUBI1 analogue-1 can be used to synthesize (4S)-PROTAC SOS1 degrader-1 (HY-144657) [1] .
|
-
- HY-176492
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 193 is an E3 ligase ligand-linker conjugate that incorporates the VHL Ligase Ligand (HY-170353) and linker (HY-176491). E3 Ligase Ligand-linker Conjugate 193 can be used for synthesis of PROTAC pan-KRAS degrader-1 (HY-176489) .
|
-
- HY-175360
-
|
|
Target Protein Ligand-Linker Conjugates
Deubiquitinase
|
Cancer
|
|
USP7 Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for USP7 (HY-175359) and a PROTAC linker, which recruits E3 ligases. USP7 Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC USP7 Degrader-1 (HY-175358) .
|
-
- HY-183251
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL) .
|
-
- HY-176422
-
-
- HY-176530
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-amide-C4-Br incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-Me-amide-C4-Br can be used to design PROTAC, such as PROTAC ERK5 degrader-1 (HY-176528) .
|
-
- HY-182298
-
-
- HY-175348
-
-
- HY-183440
-
|
|
PROTAC Linkers
|
Inflammation/Immunology
|
|
Amine-C2-piperazine-C4-OH is a flexible alkyl linker component that can be used in the synthesis of PROTAC ALK5 Degrader-1 (HY-183785). Amine-C2-piperazine-C4-OH can be applied to the research of pulmonary fibrosis .
|
-
- HY-163959
-
|
|
PNPLA3
|
Metabolic Disease
Cancer
|
|
PF-07853578 is an orally active PNPLA3 modulator. PF-07853578 significantly reduces human PNPLA3-I148M protein levels and effectively decreases hepatic triglyceride content by reducing this mutant protein. PNPLA3 degrader-1 can be used in the research of liver cirrhosis and hepatocellular carcinoma .
|
-
- HY-W934539
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Lenalidomide-amide-C8-Br is an E3 ligase CRBN ligand-linker conjugate containing Lenalidomide (HY-A0003) and a linker. Lenalidomide-amide-C8-Br can be used to synthesize PROTAC PI3Kα/δ degrader-1 (HY-182083) .
|
-
- HY-175630
-
-
- HY-163647
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) .
|
-
- HY-132998
-
|
|
PROTACs
HDAC
|
Cancer
|
|
HDAC6 degrader-1 (Compound NP8) is the PROTAC degrader for HDAC6 with a DC50 of 3.8 nM in cell MM.1S .(Blue: ligand for E3 ligase Pomalidomide (HY-10984); Black: linker (HY-140213); Pink: ligand for target protein Nexturastat A (HY-16699))
|
-
- HY-181693
-
|
|
Target Protein Ligand-Linker Conjugates
|
Others
|
|
CCW16-C2-Boc is a conjugate targeting RNF4, formed by coupling the target protein ligand CCW16 (HY-143346) with a PROTAC Linker. CCW16-C2-Boc can be used to synthesize the PROTAC degrader: PROTAC RNF4 degrader-1 (HY-181693) .
|
-
- HY-130712
-
|
|
PROTAC Linkers
|
Cancer
|
|
NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709) .
|
-
- HY-175374
-
|
|
Target Protein Ligand-Linker Conjugates
RIP kinase
|
Cancer
|
|
RIPK1 ligand-Linker Conjugate-1 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for RIPK1 (HY-175371) and a PROTAC linker (HY-175373), which recruits E3 ligases. RIPK1 ligand-Linker Conjugate-1 can be used for synthesis of PROTAC RIPK1 Degrader-1 (HY-175370) .
|
-
- HY-32717
-
|
6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-ethoxyquinoline-3-carbonitrile
|
Ligands for Target Protein for PROTAC
|
Infection
|
|
DH03 (6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-ethoxyquinoline-3-carbonitrile) is a SARS-CoV-2 M Pro ligand. DH03 can be used as a Ligand for Target Protein for PROTAC synthesis, such as PROTAC SARS-CoV-2 Degrader-1 (HY-174233) .
|
-
- HY-180179
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
BLIMP-1 Ligand-Linker Conjugate 1 is a conjugate of BLIMP-1 Ligand-1 (HY-180178) and Linker (HY-180180). BLIMP-1 ligand-Linker Conjugate 1 can be coupled with CRBN ligand-881 (HY-W442918) to form PROTAC BLIMP-1 degrader-1 (HY-180177) .
|
-
- HY-W937057
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate that incorporates a VHL ligand 2 (HY-112078) and linker 10-bromoheptanoic acid. (S,R,S)-AHPC-Me-10-bromodecanoic acid can be used for synthesis of PROTAC PI3Kδ degrader-1 (HY-176239) .
|
-
- HY-W068828
-
|
4,9-Dioxa-1,12-dodecanediamine
|
PROTAC Linkers
|
Others
|
|
1,4-Butanediol bis(3-aminopropyl) ether (4,9-Dioxa-1,12-dodecanediamine) is a PROTAC linker. Pent-4-yn-1-ol can be used to synthesize PROTAC molecules (e.g., PROTAC GSK-3β Degrader-1 (HY-149845)) .
|
-
- HY-182086
-
|
|
Ligands for Target Protein for PROTAC
PI3K
|
Cancer
|
|
Copanlisib-NH is a PI3Kα/δ ligand. Copanlisib-NH can be used as a ligand for target protein for PROTAC to develop and design degraders of PROTAC PI3Kα/δ, such as PROTAC PI3Kα/δ degrader-1 (HY-182083). Copanlisib-NH can be used in breast cancer research .
|
-
- HY-128414
-
|
|
Ligands for Target Protein for PROTAC
Ras
|
Cancer
|
|
KRAS G12C-IN-72 (Example 571) is a KRAS G12C inhibitor. KRAS G12C-IN-72 can be used as a target protein ligand to synthesize PROTACs, such as KRAS degrader-1 (HY-153880). KRAS G12C-IN-72 can be used in cancer research .
|
-
- HY-180178
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
BLIMP-1 ligand-1 (Compound 56) is a BLIMP-1 ligand. BLIMP-1 ligand-1 can be used as a ligand for target protein for PROTAC to develop and design degraders of PROTAC BLIMP-1, such as PROTAC BLIMP-1 degrader-1 (HY-180177). BLIMP-1 ligand-1 can be used in multiple myeloma research .
|
-
- HY-129776
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-129775
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-185545
-
|
|
Ligands for Target Protein for PROTAC
Trk Receptor
|
Cancer
|
|
NTRK1-ligand-1 (Compound 15) is a NTRK1 ligand. NTRK1-ligand-1 serves as a Ligand for Target Protein for PROTAC, which is applicable to the development and design of PROTAC NTRK1 degraders, such as PROTAC NTRK1 degrader-1 (HY-181052). NTRK1-ligand-1 can be used in the research of solid tumors .
|
-
- HY-111671
-
|
SOS1 activator 1
|
SOS1
Ras
PERK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer .
|
-
- HY-130991A
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 6 formate incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 formate can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-150839
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757) .
|
-
- HY-176421
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3K/110β degrader-1 (J-9) is a PROTAC based PI3K/110β degrader (Red: PI3K/110β inhibitor (HY-75124), black: linker, Blue: E3 ligase ligand) .
|
-
- HY-130822
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-130823
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-130991
-
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Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-130815A
-
-
- HY-130815
-
-
- HY-128845
-
|
|
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other . (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
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-
- HY-130707
-
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|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .
|
-
- HY-131386A
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM .
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-
- HY-131386
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
BMS-1166-N-piperidine-CO-N-piperazine incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM .
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-
- HY-161709
-
|
|
Ligands for Target Protein for PROTAC
FLT3
CDK
|
Cancer
|
|
FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708) .
|
-
- HY-174430
-
|
|
Ligands for Target Protein for PROTAC
JAK
|
Cancer
|
|
WWQ-131 is a potent selective JAK2 inhibitor with an IC50 of 2.56 nM. WWQ-131 shows >252-fold selectivity over JAK1, JAK3, and TYK2. WWQ-131 exhibits antiproliferative activity against cancer cells. WWQ-131 is the ligand for target protein for PROTAC JAK2 degrader-1 (HY-174428). WWQ-131 can be used for the research of myeloproliferative neoplasms (MPNs) .
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-
- HY-174235
-
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E3 Ligase Ligand-Linker Conjugates
|
Infection
|
|
Thalidomide-OCH2-amide-PEG2-C2-Boc is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-OCH2-amide-PEG2-C2-Boc can be used to synthesize PROTAC SARS-CoV-2 Degrader-1 (HY-174233) .
|
-
- HY-168190
-
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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))
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-
- HY-182978
-
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E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Pomalidomide-C3-O-C4-O-C3-NH2 is an E3 ligase ligand-linker conjugate that contains Pomalidomide (HY-10984). Pomalidomide-C3-O-C4-O-C3-NH2 can be used for the synthesis of PROTACs targeting glycogen synthase kinase 3β (GSK-3β), such as PROTAC GSK-3β Degrader-1 (HY-149845) .
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-
- HY-125876
-
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PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker;Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
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-
- HY-181134
-
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PROTACs
|
Cancer
|
|
PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research .
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-
- HY-130619
-
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PROTAC Linkers
|
Cancer
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|
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins .
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-
- HY-131187
-
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|
Ligands for Target Protein for PROTAC
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Cancer
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|
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1 . BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .
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-
- HY-W877997
-
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E3 Ligase Ligand-Linker Conjugates
Drug Derivative
|
Cancer
|
|
Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer .
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-
- HY-130984
-
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PROTAC Linkers
|
Cancer
|
|
Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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-
- HY-168694
-
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 147 is a conjugate of E3 ligase ligand and PROTAC Linker, which can be used to synthesize BRD9 Degrader-1 (HY-156401) (Compound 13-7) . E3 Ligase Ligand-linker Conjugate 147 is composed of the E3 ligase ligand BRD9 ligand-7 (HY-168695) and the PROTA linker 2-((1R,5S,6s)-3-Azabicyclo[3.1.0]hexan-6-yl)ethan-1-ol (HY-W763939).
|
-
- HY-185121
-
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PROTACs
CDK
Caspase
|
Cancer
|
|
PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research .
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-
- HY-176823
-
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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)) .
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-
- HY-108369R
-
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Reference Standards
PROTAC Linkers
|
Cancer
|
|
Azido-PEG1-CH2CO2H (Standard) is the analytical standard of Azido-PEG1-CH2CO2H (HY-108369). This product is intended for research and analytical applications. Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 . Azido-PEG1-CH2CO2H is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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-
- HY-173469
-
|
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c-Myc
|
Cancer
|
|
MTP3 ligand-1 is a MTP3 ligand for PROTAC MTP3 degrade-1 (HY-173467). PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader .
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-
- HY-160531
-
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Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF1-degrader-1 (Compound 9-B) is a IKZF1 molecular glue degrader with the DC50 value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors .
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-
- HY-162723
-
|
|
PROTACs
AP-1
|
Cancer
|
|
FOSL1 degrader 1 is a FOSL1 PROTAC degrader with a DC50 of 2.3 μM. FOSL1 degrader 1 induces proteasomal degradation of FOSL1. FOSL1 degrader 1 eliminates cancer stem cells in head and neck squamous cell carcinoma. FOSL1 degrader 1 suppresses head and neck squamous cell carcinoma tumorigenesis. FOSL1 degrader 1 can be used for the research of head and neck squamous cell carcinoma .
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-
- HY-179384
-
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ACSL Family
PROTACs
Ferroptosis
Glutathione Peroxidase
Transferrin Receptor
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer .
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-
- HY-144624
-
|
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PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
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-
- HY-162608
-
|
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PROTACs
JAK
STAT
|
Cancer
|
|
PROTAC JAK1 degrader 1 is a JAK1 PROTAC degrader with a DC50 of 214 nM and an IC50 of 5.2 nM. PROTAC JAK1 degrader 1 inhibits the downstream JAK-STAT signaling pathway by degrading JAK1. PROTAC JAK1 degrader 1 exhibits antiproliferative activity in cells. PROTAC JAK1 degrader 1 can be used for research on leukemia .
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-
- 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 .
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-
- HY-162665
-
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Histone Methyltransferase
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Others
|
|
WIZ degrader 1 (Compound 141) is a degrader for widely interspaced zinc finger motifs (WIZ) with an AC50 of 2 nM. WIZ degrader 1 induces the expression of fetal hemoglobin (HbF) with an EC50 of 6 mM. WIZ degrader 1 is used in research of inherited blood disorders .
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-
- HY-180276
-
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HyT
PARP
Drug Derivative
Autophagy
|
Cancer
|
|
PARP1 degrader 1 (Compound 2c) is a comparatively potent PARP1 HyT degrader (DC50: 618 nM for intracellular PARP-1). PARP1 degrader 1 is also a HyT-Olaparib (HY-10162) conjugate. PARP1 degrader 1 induces UPR/autophagy, thus facilitating the degradation of PARP-1. PARP1 Degrader 1 can be used in the research of cancer .
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-
- HY-130245A
-
|
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PCSK9
|
Metabolic Disease
|
|
(R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
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-
- HY-181287
-
|
|
PROTACs
CCR
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease .
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-
- HY-155113
-
|
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PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 is a selective PROTAC Hsp90α degrader with a DC50 of 0.295 μM. PROTAC Hsp90α degrader 1 exhibits antitumor activity with low toxic side effects. PROTAC Hsp90α degrader 1 can be used for the research of breast cancer .
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-
- HY-163814
-
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Molecular Glues
CDK
|
Cancer
|
|
CDK2 degrader 1 (Compound 3) is a selective CDK2 molecular glue degrader with a Dmax (CDK2) of > 80% and a Ki (CRBN) > 1 μM. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers .
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-
- HY-155582
-
|
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Src
|
Cancer
|
|
BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). BLK degrader 1 shows anticancer activity in several B-lymphoid cell lines .
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-
- HY-179582
-
|
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PROTACs
Glycosidase
|
Cancer
|
|
PROTAC DNPH1 Degrader 1 is a potent PROTAC DNPH1 degrader with a DC50 of 28 nM. PROTAC DNPH1 Degrader 1 mediates proteasome- and VHL-dependent DNPH1 knockdown, drives DNPH1 ubiquitination and proteasomal degradation. PROTAC DNPH1 Degrader 1 can be used for the research of brca1 mutant cancer .
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-
- HY-174138
-
|
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NF-κB
|
Inflammation/Immunology
|
|
NF-κB degrader 1 (Compound MD-1) is a NF-κB1 p105 subunit degrader. NF-κB degrader 1 shows anti-inflammatory activity (IC50 for inhibiting TNF-α is 2.02 μM, and for inhibiting NO is 5.40 μM). NF-κB degrader 1 induces p105 degradation dependent on the Cullin-RING ligase (CRL) SCFBTCP, suppressing NF-κB transcriptional activity. NF-κB degrader 1 is promising for research of inflammation-related diseases .
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-
- HY-141482
-
|
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E1/E2/E3 Enzyme
|
Cancer
|
|
WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects .
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-
- HY-175849
-
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HyT
Anaplastic lymphoma kinase (ALK)
Apoptosis
STAT
|
Cancer
|
|
ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .
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-
- HY-162930
-
|
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PROTACs
METTL3
|
Cancer
|
|
PROTAC METTL3 degrader 1 is a VHL-based PROTAC METTL3 degrader (DC50: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC50 value of 341 nM. PROTAC METTL3 degrader 1 can be used for the research of acute myeloid leukemia and gastric cancer .
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-
- HY-159592
-
|
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PROTAC Linkers
|
Cancer
|
|
Piperazine-Pyrimidine-Cyclohexane-COOEt is a PROTAC linker. Piperazine-Pyrimidine-Cyclohexane-COOEt can be used in the synthesis of PROTAC SMARCA2/4-degrader-1 (HY-159452) .
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-
- HY-180277
-
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PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC50 of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC50 > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML) .
|
-
- HY-180798
-
|
|
HyT
Bcr-Abl
|
Cancer
|
|
BCR-ABL degrader 1 (Compound 23) is a HyT-based BCR-ABL degrader with a DC50 of 19.9 μM. BCR-ABL degrader 1 can be used in the research of chronic myeloid leukemia .
|
-
- HY-157458
-
|
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ATTECs
Phosphodiesterase (PDE)
Autophagy
|
Cancer
|
|
PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .
|
-
- HY-172882
-
|
|
Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF2-degrader 1 (Compound 31) is a IKZF2 molecular glue degrader, with an DC50 of 0.5 nM. IKZF2-degrader 1 has minimal CK1α degradation activity relatively (DC50: 210 nM). IKZF2-degrader 1 can be used for research of IKZF2-dependent cancers .
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-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomesOsimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
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-
- HY-152263
-
|
|
Hsp-targeting Chimeras
CDK
Apoptosis
|
Cancer
|
|
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- 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))
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-
- HY-179657
-
|
|
PROTACs
MALT1
Histone Acetyltransferase
|
Neurological Disease
|
|
PROTAC MLT Degrader 1 (M-PRORAC) is an asymmetric dual-functional degrader based on MLT PROTAC. PROTAC MLT Degrader 1 significantly reduces the protein level of p300 in the cell. PROTAC MLT Degrader 1 can be used in Alzheimer's disease research (pink: MLT ligand (HY-B0075); blue: CRBN ligand (HY-41547); black: linker (HY-140208)) .
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-
- HY-173470
-
|
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E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
MTP3 Ligand-linker Conjugate 1 is a conjugate of the MTP3 ligand and the linker. MTP3 Ligand-linker Conjugate 1 can be used for synthesis of PROTAC MTP3 degrade-1 (HY-173467) .
|
-
- HY-137343
-
-
- HY-161796A
-
-
- HY-179308
-
|
|
Ligands for Target Protein for PROTAC
RET
|
Cancer
|
|
RET ligand-5 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC RET Degrader 1 (HY-178964). PROTAC RET Degrader 1 is a potent RET PROTAC degrader with anti-tumor activity .
|
-
- HY-173467
-
|
|
PROTACs
c-Myc
|
Cancer
|
|
PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader (Red: MYC inhibitor (HY-173469), black: linker (HY-W008296), Blue: E3 ligase ligand (HY-14658)) .
|
-
- HY-162896
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
And1 degrader 1 (Compound A15) is a degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), which can significantly induce the degradation of And1 in NSCLC cells. And1 degrader 1 (5 μM) combined with Olaparib (HY-10162) (1 μM) effectively inhibits the proliferation of A549 and H460 cells. And1 degrader 1 can be used in cancer research .
|
-
- HY-119932
-
|
|
PROTACs
FAK
Akt
|
Cancer
|
|
PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC50 of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor. (Pink: Fak ligand (HY-44146); Black: Linker (HY-44141); Blue: VHL ligand 1 (HY-125845)) .
|
-
- HY-162307
-
|
|
PROTACs
Keap1-Nrf2
|
Cancer
|
|
Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC50 of 0.1-1 μM in huH1 cells. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively. Nrf2 degrader 1 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer .
|
-
- HY-163786
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6 degrader 1 is a CDK4/CDK6 PROTAC degrader, with DC50 values of 10.5 nM and 2.5 nM, respectively. PROTAC CDK4/6 degrader 1 inhibits the proliferation of Jurkat cells (IC50 = 0.18 μM), arrests the cell cycle at the G1 phase, and induces apoptosis. PROTAC CDK4/6 degrader 1 can be used for cancer research.
|
-
- HY-170595
-
|
|
PROTACs
MDM-2/p53
c-Myc
MAP3K
|
Cancer
|
|
PROTAC LZK degrader 1 (Compound 21A) is a PROTAC that targets the degradation of LZK (Leucine Zipper Kinase, encoded by MAP3K13). PROTAC LZK degrader 1 (10 μM) promotes the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. PROTAC LZK degrader 1 can be used in cancer research. PROTAC LZK degrader 1 consists of an E3 ligase ligand (blue part, HY-112078), a target protein ligand (red part, HY-170596), and a linker (black part, HY-W019543)[1].
|
-
- HY-169077
-
|
|
Molecular Glues
IKZF Family
|
Cancer
|
|
IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 .
|
-
- HY-175976
-
|
|
Akt
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Akt3 ligand-1 is an Akt3 inhibitor (IC50 = 0.1 nM) and a ligand for the target protein for PROTAC (Akt3). Akt3 ligand-1 can be used to synthesize PROTAC Akt3 Degrader-1(HY-175975) .
|
-
- HY-161168
-
|
|
CDK
|
Cancer
|
|
Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM. Cyclin K degrader 1 has an affinity for cyclin K that is ~500-fold higher than its affinity for CDK12 .
|
-
- HY-168950
-
|
|
Annexin A
|
Cancer
|
|
ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI=96%) .
|
-
- HY-142925
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11) .
|
-
- HY-162098
-
|
|
PROTACs
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
|
-
- HY-W110929
-
-
- HY-W142446
-
-
- HY-N8180
-
|
|
Others
|
Others
|
|
Silyamandin is a flavonolignan compound. Silydianin can form Silyamandin through oxidative degradation .
|
-
- HY-161176
-
|
|
PROTACs
Ras
ERK
|
Cancer
|
|
PROTAC KRAS G12D degrader 1 is a selective PROTAC KRAS G12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRAS G12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRAS G12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)) .
|
-
- HY-178065
-
|
|
PROTACs
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)) .
|
-
- HY-179602
-
|
|
PROTACs
11β-HSD
|
Metabolic Disease
|
|
PROTAC 11β-HSD1 Degrader 1 is a highly efficient PROTAC targeting 11β-HSD1 (Hydroxysteroid 11-beta dehydrogenase 1). PROTAC 11β-HSD1 Degrader 1 demonstrates ubiquitin-proteasome-dependent degradation of 11β-HSD1. PROTAC 11β-HSD1 Degrader 1 can be used for the study of type 2 diabetes mellitus (T2DM) .
|
-
- HY-146368
-
|
|
PROTACs
VEGFR
|
Cancer
|
|
PROTAC VEGFR-2 degrader-1(PROTAC-1), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM) .
|
-
- HY-155398
-
-
- HY-155397
-
-
- HY-162318
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
|
-
- HY-130245
-
|
|
PCSK9
|
Metabolic Disease
|
|
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
|
-
- HY-162318A
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
|
-
- HY-163640
-
-
- HY-114323
-
|
|
PROTACs
FLT3
Apoptosis
STAT
MEK
ERK
|
Cancer
|
|
PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)) .
|
-
- HY-176476
-
|
|
Epigenetic Reader Domain
FKBP
|
Cancer
|
|
BRD4/FKBP12 degrader-1(a1d) is a BRD4/FKBP12 degrader with anti-cancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176501, linker: HY-140212) .
|
-
- HY-175830
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
PROTAC AURKA degrader 1 (Compound A16 + X7) is a Aurora kinase A (AURKA) PROTAC degrader. PROTAC AURKA degrader 1 can be used for cancers research . Pink: AURKA ligand (HY-175827); Blue: CRBN ligase ligand (HY-W867704); Black: linker (HY-132208)
|
-
- HY-159593
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo is an E3 Ligase Ligand-Linker Conjugate. Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo can be used to synthesize PROTAC SMARCA2/4-degrader-1 (HY-159452) .
|
-
- HY-146384
-
|
|
CRM1
|
Cancer
|
|
CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer .
|
-
- HY-159452
-
|
|
PROTACs
|
Cancer
|
|
SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
|
-
- HY-169343
-
|
|
Molecular Glues
|
Cancer
|
|
FIZ1 degrader 1 (compound 1) is an IMiD-based molecular glue degrader targeting FIZ1 .
|
-
- HY-W777618
-
|
(+)-Cinerin II
|
Others
|
Infection
|
|
Cinerin II ((+)-Cinerin II) is a pyrethrin ester found in Chrysanthemum cinerariifolium. Cinerin II is a safe pesticide with rapid degradation .
|
-
- HY-157582
-
|
|
EGFR
|
Others
|
|
MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing degradation .
|
-
- HY-158767
-
|
|
Drug Derivative
|
Others
|
|
Dehydro amlodipine fumarate is a derivative of Dehydro amlodipine and is one of the forced degradation products of Dehydro amlodipine during oxidation and acid degradation .
|
-
- HY-W777613
-
|
(-)-Jasmolin I
|
Others
|
Infection
|
|
Jasmolin I ((-)-Jasmolin I) is a pyrethrin ester found in Chrysanthemum cinerariifolium. Jasmolin I is a safe pesticide with rapid degradation .
|
-
- HY-178452
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)) .
|
-
- HY-178964
-
|
|
PROTACs
RET
|
Cancer
|
|
PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
|
-
- HY-169235
-
-
- HY-161597
-
|
|
PROTACs
DYRK
|
Cancer
|
|
PROTAC DYRK2 degrader 1 is a DYRK2 PROTAC degrader with DC50 values of 1.607 μM (MDA-MB-231 cells) and 3.265 μM (HeLa cells), respectively. PROTAC DYRK2 degrader 1 induces DYRK2 degradation via the ubiquitin-proteasome system. It is applicable to the research of triple-negative breast cancer and cervical cancer .
|
-
- HY-178067
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Phthalimidinoglutarimide-5-piperazine-COC2-alkynes is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC BCL-xL/BCL-w Degrader 1 (HY-178066). PROTAC BCL-xL/BCL-w Degrader 1 is a potent BCL-xL/BCL-w PROTAC degrader with anti-cancer activity .
|
-
- HY-159607A
-
|
|
PROTACs
|
Others
|
|
PRT3789 epimer is an epimer of PRT3789 (HY-159607). PRT3789 is a selective SMARCA2 PROTAC degrader .
|
-
- HY-168725
-
|
|
PROTACs
Kinesin
Apoptosis
|
Cancer
|
|
PROTAC KSP degrader 1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP degrader 1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP degrader 1 exhibits antitumor efficacy in mouse model . (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
|
-
- HY-163985
-
|
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker:HY-163986) .
|
-
- HY-178069
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-PEG3-NHBoc is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC G9a/GLP degrader 1 (HY-178065). PROTAC G9a/GLP degrader 1 is a potent G9a/GLP PROTAC degrader with anti-cancer activity .
|
-
- HY-150400
-
|
|
PROTACs
WDR5
|
Cancer
|
|
XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) PROTAC degrader .
|
-
- HY-163989
-
|
|
PROTAC Linkers
|
Cancer
|
|
N-Ethylheptanamide is a PROTAC linker. N-Ethylheptanamide can be used in synthesis PROTAC FGFR2 degrader 1 (HY-163985) .
|
-
- HY-130617
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity .
|
-
- HY-168654
-
|
|
Wee1
|
Cancer
|
|
WEE1 degrader 1 (Compound 10) is a CRBN-dependent molecular glue degrader of WEE1 and casein kinase 1α (CK1α) with sub-2 nM DC50 values for both targets. WEE1 degrader 1 can be used for the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, diffuse large b cell lymphoma .
|
-
- HY-178118
-
|
|
PROTACs
PDI
|
Cancer
|
|
PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation . Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
|
-
- HY-168488
-
-
- HY-111593
-
|
|
PROTACs
|
Cancer
|
|
Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC , consists of two ligands of von Hippel-Lindau.
|
-
- HY-NP0221
-
|
|
Transferrin Receptor
|
Inflammation/Immunology
|
|
Rabbit Transferrin is the major iron-containing protein in plasma, responsible for transporting iron absorbed from the digestive tract and iron released by erythrocyte degradation .
|
-
- HY-153042
-
-
- HY-162282
-
|
|
PROTACs
DNA Methyltransferase
|
Cancer
|
|
PROTAC METTL3-14 degrader 1 (compound 30) is a PROTAC degrader of METTL3-14. PROTAC METTL3-14 degrader 1 shows a 50% or higher degradation of METTL3 and/or METTL14(Pink: Ligand for target protein (HY-115717); Black: Linker (HY-168686); Blue: Ligand for E3 ligase (HY-10984)) .
|
-
- HY-131230
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1 (HY-114323). PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM .
|
-
- HY-178066
-
|
|
Bcl-2 Family
PROTACs
|
Cancer
|
|
PROTAC BCL-xL/BCL-w Degrader 1 (Compound 44) is a BCL-xL/BCL-w PROTAC degrader. PROTAC BCL-xL/BCL-w Degrader 1 has significant anticancer activity with reduced on-target platelet toxicity . Pink: BCL-xL/BCL-w ligand (HY-10087); Blue: CRBN ligase ligand (HY-163233); Black: linker (HY-Y1230)
|
-
- HY-159494
-
|
|
PROTACs
Epoxide Hydrolase
|
Metabolic Disease
|
|
sEH-degrader-1 (Compound 8) serves as an inhibitor for sEH, with IC50 values of 3.8 nM and 210 nM against hsEH and msEH respectively. sEH-degrader-1 can effectively degrade sEH in mouse liver and brown adipose tissue (Red: UC-1728 (HY-114266), black: linker (HY-W248248), Blue: Thalidomide-5-piperazine (HY-W834174)) .
|
-
- HY-169370
-
-
- HY-139340
-
|
|
PROTACs
|
Others
|
|
Photo-lenalidomide-acid (compound 3) is a photacts consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest and enable optical control of protein degradation .
|
-
- HY-113136
-
|
N1-Methylguanosine
|
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine (N1-Methylguanosine) is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
|
-
- HY-NP200
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Keratin azure can be used to monitor the degradation of (β)-keratin. Keratin azure can be used as a substrate in keratin assays to assess keratinase degradation .
|
-
- HY-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
-
- HY-111758
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity .
|
-
- HY-111594
-
|
|
PROTACs
|
Cancer
|
|
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3 .
|
-
- HY-113472
-
|
|
Drug Metabolite
|
Others
|
|
N-Methyl-4-pyridone-3-carboxamide (compound 4PY) is a final product of nicotinamide adenine dinucleotide (NAD) degradation .
|
-
- HY-118653
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation .
|
-
- HY-141551B
-
|
|
Drug Isomer
|
Others
|
|
(R)-GNE-274 is a enantiomer of GNE-274. GNE-274 is a non-degrader that is structurally related to GDC-0927 (estrogen receptor degrader) .
|
-
- HY-120722
-
TCH-165
2 Publications Verification
|
Proteasome
|
Cancer
|
|
TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation .
|
-
- HY-44146
-
-
- HY-130640
-
-
- HY-168897
-
-
- HY-169134
-
|
|
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) is a targeted degrader of PROTAC for 20S proteasome subunit β5, with a DC50 value of 0.11 μM in FaDu cells. PROTAC 20S proteasome subunit β5 degrader 1 disrupts the cell cycle, promotes apoptosis, and inhibits cell proliferation and migration in both FaDu and KM3/BTZ cells. PROTAC 20S proteasome subunit β5 degrader 1 can be used to study the resistance of pharyngeal cancer and multiple myeloma to Bortezomib (HY-10227) (Pink: Target protein ligand (HY-10227); Blue: E3 ligase ligand (HY-103596); Black: Linker (HY-169142)) .
|
-
- HY-157839
-
|
|
PROTACs
α-synuclein
Tau Protein
|
Neurological Disease
|
|
PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with KDs of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)) .
|
-
- HY-168540
-
|
|
PROTACs
Mps1
Aurora Kinase
|
Cancer
|
|
PROTAC MPS1 degrader 1 (Compound 19) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA and AURKB, with DC50s of 17.7, 108.7 and 570.3 nM, respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168542); Black: linker (HY-W141926); Blue: ligand for E3 ligase (HY-10984) .
|
-
- HY-168896
-
|
|
CDK
ATTECs
|
Cancer
|
|
CDK9 autophagic degrader 1 (Compound 28) is a ATTEC degrader that can be used to degrade CDK9 and also affects the levels of the associated Cyclin T1. CDK9 autophagic degrader 1 shows over 80% CDK9 inhibition rate at 100 nM . ( Pink: LC3B ligand (HY-168897); Black: linker (HY-W017758); Blue: target protein ligand (HY-10008); linker + target protein ligand (HY-168898))
|
-
- HY-175611
-
-
- HY-W017389
-
-
- HY-159733
-
-
- HY-114406
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
|
-
- HY-180280
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
KLHDC2 ligand 3 is an E3 ligase ligand. KLHDC2 ligand 3 can be used for the synthesis of PROTAC CDK6 Degrader 1 (HY-180277) .
|
-
- HY-W248248
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 9-aminononanoate is a PROTAC linker. tert-Butyl 9-aminononanoate can be used in synthesis PROTAC sEH-degrader-1 (HY-159494) .
|
-
- HY-162973
-
-
- HY-W781976
-
|
XDE-175-J
|
Insecticide
|
Infection
|
|
Spinetoram J (XDE-175-J) is the major component of Spinetoram. Spinetoram is a green, highly effective and broad-spectrum insecticide, which is friendly to the environment, humans and animals, and degradable .
|
-
- HY-161598
-
-
- HY-169094
-
-
- HY-W749852
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Xanthine sodium, 98%, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, 98% also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-161575
-
-
- HY-185595
-
|
|
Drug Intermediate
|
Others
|
|
N,3-BisBoc-L-Histidine is a Hyt hydrophobic group. N,3-BisBoc-L-Histidine can be used in the synthesis of BCR-ABL degrader 1 (HY-180798).
|
-
- HY-175689
-
-
- HY-145514A
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12 F36V-selective degrader .
|
-
- HY-W719881
-
|
|
Herbicide
|
Others
|
|
Isocarbamid is an imidazolinone herbicide. Isocarbamid is sensitive to changes in soil temperature, and its degradation is highly dependent on microbial activity; therefore, low temperatures significantly slow down or even completely inhibit its degradation .
|
-
- HY-W749852A
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Xanthine sodium, for cell culture, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, for cell culture also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-175600
-
-
- HY-135345
-
|
|
PROTACs
FKBP
|
Cancer
|
|
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
|
-
- HY-168898
-
-
- HY-168487
-
|
|
DNA/RNA Synthesis
PROTACs
WDR5
|
Others
|
|
PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A) .
|
-
- HY-158767R
-
|
|
Drug Derivative
Reference Standards
|
Others
|
|
Dehydro amlodipine (fumarate) (Standard) is the analytical standard of Dehydro amlodipine (fumarate). This product is intended for research and analytical applications. Dehydro amlodipine fumarate is a derivative of Dehydro amlodipine and is one of the forced degradation products of Dehydro amlodipine during oxidation and acid degradation .
|
-
- HY-175665
-
|
|
Ligands for E3 Ligase
|
Others
|
|
LC3 liagnd-2 is an E3 ligase ligand. LC3 liagnd-2 can be used for synthesis of PROTAC PDEδ autophagic degrader 1 (HY-157458) .
|
-
- HY-175601
-
|
|
IKZF Family
Molecular Glues
|
Others
|
|
DD-04-038 is a molecular glue degrader. DD-04-038 induces proteins (such as IKZF1/3, ZBED3 and PATZ1) to bind to CRBN, promoting their ubiquitination and degradation .
|
-
- HY-168702
-
-
- HY-133799
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C7-COOH is a synthesized E3 ligase cereblon ligand-linker conjugate. Pomalidomide-C7-COOH is an intermediate for the synthesis of PROTAC BCL-XL degraders .
|
-
- HY-P2191
-
|
|
Kisspeptin Receptor
|
Endocrinology
|
|
KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation .
|
-
- HY-149917
-
|
|
PROTACs
Itk
|
Cancer
|
|
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389) .
|
-
- HY-159660
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 31 is a ligand for E3 ubiquitinase. E3 ligase Ligand 31 can be used to synthesize PTOTAC HSD17B13 degrader 1 (HY-159651) .
|
-
- HY-160438A
-
|
|
Survivin
|
Cancer
|
|
PBX-7011 mesylate is an active Camptothecin (HY-16560) derivative. PBX-7011 can bind to the DDX5 protein in cells, thereby inducing cell death through DDX5 protein degradation .
|
-
- HY-169158
-
-
- HY-158684A
-
|
|
Drug Isomer
|
Cancer
|
|
(4R,5S)-YX-02-030 is an isomer of YX-02-030 (HY-158684). YX-02-030 is a PROTAC MDM2 degrader .
|
-
- HY-168288
-
-
- HY-180278
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK6 ligand 2 is a ligand for target CDK6 protein for PROTAC. PROTAC CDK6 ligand 2 can be used for the synthesis of PROTAC CDK6 Degrader 1 (HY-180277) .
|
-
- HY-W016087
-
|
|
PROTAC Linkers
|
Cancer
|
|
Monoethyl pimelate is a PROTAC linker, which refers to the alkyl/ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader .
|
-
- HY-160438
-
|
|
Survivin
|
Cancer
|
|
PBX-7011 is an active camptothecin (HY-16560) derivative. PBX-7011 can bind to the DDX5 protein in cells, thereby inducing cell death through DDX5 protein degradation .
|
-
- HY-173599
-
|
|
PNPLA3
|
Cancer
|
|
NUV-244 is a PNPLA3 I148M degrader. NUV-244 reduces PNPLA3 I148M levels on lipid droplets via BFAR-mediated ubiquitin-proteasome degradation .
|
-
- HY-145514B
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12 F36V-selective degrader .
|
-
- HY-130770
-
|
|
PROTAC Linkers
|
Cancer
|
|
Ald-CH2-PEG3-CH2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of SGK3 kinase PROTAC degrader .
|
-
- HY-157592
-
-
- HY-179603
-
-
- HY-179307
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 77 is a CRBN type E3 ubiquitin ligase ligand. E3 ligase Ligand 77 can be used for synthesizing PROTAC, such as PROTAC RET Degrader 1 (HY-178964) .
|
-
- HY-113136R
-
|
N1-Methylguanosine (Standard)
|
Endogenous Metabolite
Reference Standards
|
Cancer
|
|
1-Methylguanosine (Standard) is the analytical standard of 1-Methylguanosine. This product is intended for research and analytical applications. 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
|
-
- HY-W802197
-
|
|
Others
|
Others
|
|
D-Xylose 2,3,4,5-tetraacetate is a competitive substrate analog targeting acetyl xylan esterases (AXEs). D-Xylose 2,3,4,5-tetraacetate is promising for research of lignocellulosic biomass degradation .
|
-
- HY-148523
-
|
|
Molecular Glues
CDK
|
Cancer
|
|
HQ005 is a potent CCNK degrader with an DC50 value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .
|
-
- HY-168687
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 137 is the linker and E3 ligase ligand for the PROTAC METTL3-14 degrader 1 (HY-162282), which can be used for research on acute myeloid leukemia .
|
-
- HY-169395
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-CO-PEG-C2-iodine is an E3 ligase (VHL) ligand-linker conjugate, and can be used for synthesis of PROTACs, such as PROTAC FAK degrader 1 (HY-119932)
|
-
- HY-124449
-
|
ME-5343
|
TRP Channel
|
Others
|
|
Afidopyropen (ME-5343) is an Afidopyropen targets sucking insects such as whiteflies, aphids, and leafhoppers by acting on the Nanchung (Nan) and Inactive (Iav) encoding gene of insects, and affecting TRPV channel. Afidopyropen can be used for many crops for its degradability .
|
-
- HY-178512
-
|
|
PROTAC Linkers
|
Cancer
|
|
Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is a PROTAC linker can be used in the synthesis of PROTACs, such as PROTAC CDK4/6/9 degrader 1 (HY-178452) .
|
-
- HY-D2259
-
|
|
E1/E2/E3 Enzyme
Ligands for E3 Ligase
|
Others
|
|
PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
|
-
- HY-44141
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 3-(2-iodoethoxy)propanoate is a PROTAC linker, which refers to the PEG composition. tert-Butyl 3-(2-iodoethoxy)propanoate can be used in the synthesis of PROTAC FAK degrader 1 (HY-119932) .
|
-
- HY-168686
-
|
|
PROTAC Linkers
|
Cancer
|
|
6-Hydroxy-1-(4-(2-hydroxyethyl) piperazin-1-yl) hexan-1-one is the linker for PROTAC METTL3-14 degrader 1 (HY-162282) .
|
-
- HY-156395
-
MN551
1 Publications Verification
|
E1/E2/E3 Enzyme
|
Cancer
|
|
MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation .
|
-
- HY-136183
-
|
VH032 phenol-alkylC6-amine dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-phenol-alkylC6-amine dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and an alkyl linker used for PROTAC degrader .
|
-
- HY-162610
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-alkyne-C4-NHBoc is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-alkyne-C4-NHBoc can be used to synthesize PROTAC JAK1 degrader 1 (HY-162608) .
|
-
- HY-175602
-
-
- HY-162327
-
|
|
PROTACs
HBV
|
Infection
|
|
PROTAC PAPD5 degrader 1 (compound 12b) inhibits both hepatitis A (HAV) and hepatitis B virus (HBV) in vitro and in vivo , with IC50 and CC50 of 10.59 μM and > 50 μM, respectively in Huh7 cells .
|
-
- HY-128839
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader .
|
-
- HY-44148
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation .
|
-
- HY-W142446S
-
-
- HY-126534A
-
|
LSN3106729 hydrochloride
|
Ligands for Target Protein for PROTAC
CDK
|
Cancer
|
|
Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
|
-
- HY-129363
-
-
- HY-126534
-
|
LSN3106729
|
Ligands for Target Protein for PROTAC
CDK
|
Cancer
|
|
Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
|
-
- HY-129363A
-
|
|
Ligands for Target Protein for PROTAC
FKBP
|
Cancer
|
|
AP1867-3-(aminoethoxy) hydrochloride, the AP1867 (HY-114434) based moiety, is a synthetic ligand for FKBP. AP1867-3-(aminoethoxy) hydrochloride can be used in the synthesis of PROTAC FKBP12 F36V degrader .
|
-
- HY-130800
-
-
- HY-159661
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 114 is an E3 ubiquitinase ligand + linker conjugate. E3 Ligase Ligand-linker Conjugate 114 can be used to synthesize PTOTAC HSD17B13 degrader 1 (HY-159651) .
|
-
- HY-159662
-
|
|
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) .
|
-
- HY-157591
-
-
- HY-130648
-
-
- HY-175827
-
-
- HY-162411
-
|
|
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 .
|
-
- HY-180547
-
|
|
PROTACs
|
Neurological Disease
|
|
MRC71 is a TRIMTAC degrader targeting Halo Tag, containing a PEG linker and chloroalkane. MRC71 selectively degrades oligomeric CAV1- and Cavin1-mEGFP-Halo over monomeric mEGFP-Halo and exhibits a characteristic hook effect concentration-dependence for degradation .
|
-
- HY-163986
-
-
- HY-183800
-
-
- HY-13822
-
|
|
SphK
Wnt
Apoptosis
|
Cancer
|
|
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation .
|
-
- 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 .
|
-
- HY-W998281
-
|
|
Drug Intermediate
|
Others
|
|
3-(4-(5-Hydroxypent-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione (Compound 15c) is an important intermediate in the synthesis of RET Degrader .
|
-
- HY-W489121
-
|
|
p62
Autophagy
|
Cancer
|
|
YTK-105 is a p62/ZZ binding domain ligand and Autophagy enhancer. YTK-105 activates p62-dependent selective macroautophagy. YTK-105 serves as an autophagy-targeting ligand (ATL) for synthesizing AUTOTAC degraders .
|
-
- HY-159651
-
|
|
PROTACs
17β-HSD
|
Cancer
|
|
PTOTAC HSD17B13 degrader 1 (compound 1) is a PROTAC targeting 17β-HSD 13 (HSD17B13). PTOTAC HSD17B13 degrader 1 is composed of PROTAC target protein ligand HSD17B13 degrader 2 (HY-159662) (red part), PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate (HY-W003696) (black part) and E3 ubiquitin ligase ligand E3 ligase Ligand 31 (HY-159660) (blue part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 114 (HY-159661) [1] .
|
-
- HY-144605
-
|
|
EGFR
PROTACs
|
Cancer
|
|
PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
|
-
- HY-113136S
-
|
N1-Methylguanosine-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine-d3 (N1-Methylguanosine-d3) is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
|
-
- HY-132288
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader .
|
-
- HY-163787
-
|
|
CDK
|
Cancer
|
|
YY173 is a dual inhibitor for CDK4 and CDK6 with IC50 of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC50 of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786) .
|
-
- HY-179061
-
|
|
Target Protein Ligand-Linker Conjugates
LAG-3
|
Cancer
|
|
LAG-3 degrader 1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as LAG-3 PROTAC-1 (HY-179060). LAG-3 PROTAC-1 is a potent LAG-3 PROTAC degrader with anti-tumor activity .
|
-
- HY-162626
-
|
|
PROTACs
FGFR
|
Cancer
|
|
FGFR2 degrader 1 (compound 28E) is a selectively PROTACS degrader of FGFR2, with the DC50 of 0.645 nM. FGFR2 plays an important role in cancer research (Pink: ligand of target protein; (HY-13304) black: linker; blue: ligand of E3 ligase) .
|
-
- HY-W017389S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Xanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Xanthine (HY-W017389). Xanthine is a plant alkaloid with mild stimulant activity of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-185594
-
|
|
Drug Intermediate
|
Others
|
|
4-(Cyclohexylbuta-1,3-diyn-1-yl)benzoic acid is a Hyt hydrophobic group. 4-(Cyclohexylbuta-1,3-diyn-1-yl)benzoic acid can be used in the synthesis of PARP1 degrader 1 (HY-180276).
|
-
- HY-W854844A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
JP-2-196 (TFA) is a molecular glue handle that can bind to the E3-ubiquitin ligases (RNF126, LRSAM1, RNF40, MID2, and RNF14) in vitro. JP-2-196 (TFA) can be used to synthesize molecular glue degraders .
|
-
- HY-170429
-
|
|
PIN1
|
Cancer
|
|
BJP-07-017-3 is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 9 nM. BJP-07-017-3 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation .
|
-
- HY-13982
-
JSH-23
Maximum Cited Publications
141 Publications Verification
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
|
-
- HY-168055
-
|
|
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 .
|
-
- HY-181288
-
-
- HY-136186
-
|
VH032-C7-amine
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-158383
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-CO-C3-PEG4-C6-NH2 is an E3 ligase ligand-linker conjugate part of PROTAC PIPIB degrader 1 (HY-158381). Pomalidomide consists of the E3 ligase ligand Pomalidomide (HY-10984) and a linker .
|
-
- HY-136186B
-
|
VH032-C7-amine hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-180279
-
|
|
Target Protein Ligand-Linker Conjugates
CDK
|
Cancer
|
|
CDK6 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that incorporates a ligand for CDK6 (HY-180278) and a linker, which recruits E3 ligases. CDK6 ligand-Linker Conjugate 1 can be used for synthesis of PROTAC CDK6 Degrader 1 (HY-180277) .
|
-
- HY-178515
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-piperazine-CO-C-azacyclohexane-C1-piperazine is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-piperazine-CO-C-azacyclohexane-C1-piperazine can be used for synthesizing PROTAC CDK4/6/9 degrader 1 (HY-178452) .
|
-
- HY-131295
-
|
|
MEK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
|
-
- HY-179230
-
|
|
PROTAC-Linker Conjugates for PAC
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 214 is an E3 ligase ligand-linker conjugate containing a Von Hippel-Lindau (VHL) ligand and a linker. E3 Ligase Ligand-linker Conjugate 214 can bind to a target protein ligand to form a PROTAC molecule, PROTAC LSD1 Degrader 1 (HY-179229) .
|
-
- HY-158381
-
|
|
PROTACs
Phosphatase
|
Metabolic Disease
|
|
PROTAC PTP1B degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader, with DC50 values of 0.2 μM (48 h) and 0.05 μM (72 h) (Red: PTP1B ligand Oleanolic acid (HY-N0156); Black: linker; Blue: CRBN ligand) .
|
-
- HY-W998310
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-C4-COOH is a conjugate of the E3 ligase VHL ligand and a linker, which can be used to synthesize PROTAC ERα Degrader-12 (HY-174453). PROTAC ERα Degrader-12 is a potent and highly selective ERα PROTAC degrader .
|
-
- HY-136187
-
|
VH032-C5-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-E70013A
-
|
EC 3.2.1.73
|
Glycosidase
|
Others
|
|
Licheninase (EC 3.2.1.73) is a glycoside hydrolase is active on the β-glucan cell wall of cereals, fungi, and seaweed. Licheninase specifically hydrolyzes β(1→4) linkages in mixed linkage β(1→3)/β(1→4)-glucans. Licheninase improves cellulose degradation .
|
-
- HY-179303
-
|
|
Ligands for Target Protein for PROTAC
Glycosidase
|
Cancer
|
|
DNPH1 ligand-1 (Compound 58) is a DNPH1 ligand. DNPH1 ligand-1 can be used as a target protein ligand (Ligands for Target Protein for PROTAC) for the development and design of PROTAC DNPH1 degraders. DNPH1 ligand-1 can be used to synthesize PROTAC DNPH1 Degrader 1 (HY-179582) .
|
-
- HY-136187A
-
|
VH032-C5-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-126534S
-
|
LSN3106729-d8
|
CDK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
|
-
- HY-114407
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
|
-
- HY-148476
-
|
|
LYTACs
|
Metabolic Disease
|
|
Tri-GalNAc-DBCO is a synthetic ligand composed of three GalNAc units connected to DBCO. Tri-GalNAc-DBCO can act as a ligand for the sialic acid-degrading protein receptor (ASGPR), and can be coupled with targeting proteins or small molecules to form GalNAc-LYTACs. Tri-GalNAc-DBCO specifically binds to ASGPR and, through receptor-mediated endocytosis, guides the coupled molecules to lysosomes for degradation .
|
-
- HY-157765
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation .
|
-
- HY-W003696
-
|
Tert-butyl 5-bromo-1,3-dihydro-2H-isoindole-2- carboxylate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 5-bromoisoindoline-2-carboxylate (Tert-butyl 5-bromo-1,3-dihydro-2H-isoindole-2- carboxylate) is a PROTAC Linker. tert-Butyl 5-bromoisoindoline-2-carboxylate can be used in synthesis PTOTAC HSD17B13 degrader 1 (HY-159651) .
|
-
- HY-168290
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide can be used in the synthesis of PROTACs, such as MS934 (HY-153863). MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader .
|
-
- HY-167701
-
|
|
Ligands for Target Protein for PROTAC
Apoptosis
Estrogen Receptor/ERR
|
Cancer
|
|
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders .
|
-
- HY-W017389R
-
|
|
Reference Standards
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Xanthine (Standard) is the analytical standard of Xanthine. This product is intended for research and analytical applications. Xanthine, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
In Vitro: A number of stimulants are derived from Xanthine including caffeine and theobromine. Xanthine is a product on the pathway of purine degradation. Xanthine is subsequently converted to uric acid by the action of the Xanthine oxidase enzyme.
|
-
- HY-13982R
-
|
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
JSH-23 (Standard) is the analytical standard of JSH-23. This product is intended for research and analytical applications. JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
|
-
- HY-N6769
-
|
Monorden
|
HSP
Bacterial
Antibiotic
Parasite
|
Infection
|
|
Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
|
-
- HY-185102
-
|
|
PROTACs
|
Cancer
|
|
ZBP1 PROTAC-1 (2a+aptamer) is a Z-DNA binding protein 1 (ZBP1) PROTAC. ZBP1 PROTAC-1 consists of a DNA aptamer (specifically binds to ZBP1) and an E3 enzyme-recruiting unit. ZBP1 PROTAC-1 combines the high specificity of DNA aptamers with the degradation-inducing capabilities of PROTACs, providing a powerful tool for targeted protein degradation .
|
-
- HY-111836
-
|
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation .
|
-
- HY-W457949
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-alkylC4-azide (Compound 2) is an azide compound containing a MIDI group and is one of the compounds used to construct a library of MIDI azide compounds. Pomalidomide 4'-alkylC4-azide is an E3 ligase ligand and linker conjugate (E3 Ligase Ligand-Linker Conjugate). Pomalidomide 4'-alkylC4-azide can be used to develop research on PROTAC degraders .
|
-
- HY-141894
-
|
|
Histone Acetyltransferase
|
Metabolic Disease
|
5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA (HY-134653) analog which contains an acetoxymethyl (AM) group. 5-Ph-IAA-AM affords an enhanced protein degradation in laid embryos. 5-Ph-IAA-AM can be used to disclosure the roles of proteins in C. elegans, in particular those that are involved in embryogenesis and development, through temporally controlled protein degradation .
|
-
- HY-180262
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK6 Degrader 2 (compound 48b), the active form of PROTAC CDK6 Degrader 1 (HY-180277), is a potent and selective PROTAC CDK6 degrader that binds strongly to KLHDC2 (KD = 0.005 μM). PROTAC CDK6 Degrader 2 functions through a KLHDC2-dependent and ubiquitin-proteasome-mediated mechanism. PROTAC CDK6 Degrader 2 can be used for cancer research .
|
-
- HY-124625
-
|
|
FAK
Target Protein Ligand-Linker Conjugates
|
Infection
Cancer
|
|
BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 is a FAK (HY-43760) ligand and linker conjugate. BI-4464 can be used to construct proteolysis targeting chimeras (PROTACs), such as PROTAC FAK degrader 4 (HY-178467). PROTAC FAK degrader 4 is a highly potent and selective FAK PROTAC degrader .
|
-
- HY-168543
-
|
|
PROTACs
Aurora Kinase
Mps1
|
Cancer
|
|
PROTAC MPS1 degrader 2 (Compound 15) is a potent degrader of monopolar spindle 1 (Mps1,TTK),AURKA and AURKB,with DC50s of 42.0,2.1 and 154.0 nM,respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168545); Black: linker (HY-N0420); Blue: ligand for E3 ligase (HY-10984) .
|
-
- HY-133046
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader . VHL Ligand-Linker Conjugates 17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-136186A
-
|
VH032-C7-amine dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine dihydrochloride is the dihydrochloride form of (S,R,S)-AHPC-C7-amine (HY-136186). (S,R,S)-AHPC-C7-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker. (S,R,S)-AHPC-C7-amine can be used for estrogen-related receptor α (ERRα) PROTAC degrader .
|
-
- HY-129619
-
|
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
|
-
- HY-130711A
-
|
VH032-C3-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
|
-
- HY-159788
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC K-Ras Degrader-4 (Compound 4) is a PROTAC degrader for KRAS that degrades KRAS G12D in GP5d and degrades KRAS G12V in cell SW620 with DC50s of 1 nM and 13 nM. PROTAC K-Ras Degrader-4 inhibits MAPK signaling pathway . (Pink: ligand for target protein pan-KRAS degrader 1 (HY-162960); Black: linker (HY-159790); Blue: ligand for E3 ligase VHL (HY-W998248))
|
-
- HY-130711
-
|
VH032-C3-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
|
-
- HY-P3171
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Acetyl-(Cys4,D-Phe7,Cys10)-a-MSH (4-13) is a melanotropin cyclic peptide. Acetyl-(Cys4,D-Phe7,Cys10)-a-MSH (4-13) ultraprolongs melanotropic activity in frog and lizard skin model with great agonisim. Acetyl-(Cys4,D-Phe7,Cys10)-a-MSH (4-13) exhibits a complete resistance to tryptic degradation .
|
-
- HY-126404
-
|
|
Environmental Pollutants
Interleukin Related
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Casein hydrolysate is an orally effective, multi-functional mixture of bioactive peptides, a hydrolysis product of casein (HY-125865), containing ACE inhibitors and immunomodulatory target regulators, among others. Casein hydrolysate releases short-chain bioactive peptides through enzymatic hydrolysis of casein, increasing cellular glutathione and catalase levels, enhancing ConA-induced IL-2 production, and exhibiting metal ion chelation, free radical scavenging, antibacterial, and mineral absorption-promoting effects. Casein hydrolysate lowers blood pressure by inhibiting angiotensin-converting enzyme (ACE) and reducing bradykinin degradation .
|
-
- HY-145177
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader . (From patent WO2017180417A1 compound s7).
|
-
- HY-144995
-
|
CDK4/6-IN-11
|
PROTACs
CDK
|
Cancer
|
|
CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader . CDK4/6-IN-11 consists of a thalidomide-based E3 ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717), a target protein ligand (red part) Palbociclib (HY-50767), and a PROTAC linker (black part) Boc-NH-C4-Br (HY-W007803). E3 ligase ligand and linker can form Thalidomide-NH-amido-C4-Br (HY-170307).
|
-
- HY-175022
-
|
|
PROTACs
IRAK
Toll-like Receptor (TLR)
Interleukin Related
|
Inflammation/Immunology
|
|
PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research . Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
|
-
- HY-130711C
-
|
VH032-C3-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .
|
-
- 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 .
|
-
- HY-130652
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach . Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D2336
-
|
|
Fluorescent Dyes
|
|
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) .
|
-
- HY-D2259
-
|
|
Fluorescent Dyes
|
|
PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W110929
-
|
Xylene blue; C.I. Acid blue 1
|
Biochemical Assay Reagents
|
|
Acid blue 1 (Xylene blue) is an anionic triarylmethane dye and substrate for photocatalytic degradation .
|
-
- HY-W749852
-
|
|
Biochemical Assay Reagents
|
|
Xanthine sodium, 98%, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, 98% also acts as an intermediate product on the pathway of purine degradation .
|
-
- HY-NP200
-
|
|
Biochemical Assay Reagents
|
|
Keratin azure can be used to monitor the degradation of (β)-keratin. Keratin azure can be used as a substrate in keratin assays to assess keratinase degradation .
|
-
- HY-W749852A
-
|
|
Biochemical Assay Reagents
|
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Xanthine sodium, for cell culture, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine sodium, for cell culture also acts as an intermediate product on the pathway of purine degradation .
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- HY-NP0221
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Biochemical Assay Reagents
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Rabbit Transferrin is the major iron-containing protein in plasma, responsible for transporting iron absorbed from the digestive tract and iron released by erythrocyte degradation .
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Product Name |
Target |
Research Area |
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- HY-P2191
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Kisspeptin Receptor
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Endocrinology
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KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation .
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- HY-169235
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- HY-P3171
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Biochemical Assay Reagents
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Others
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Acetyl-(Cys4,D-Phe7,Cys10)-a-MSH (4-13) is a melanotropin cyclic peptide. Acetyl-(Cys4,D-Phe7,Cys10)-a-MSH (4-13) ultraprolongs melanotropic activity in frog and lizard skin model with great agonisim. Acetyl-(Cys4,D-Phe7,Cys10)-a-MSH (4-13) exhibits a complete resistance to tryptic degradation .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W017389S
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Xanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Xanthine (HY-W017389). Xanthine is a plant alkaloid with mild stimulant activity of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation .
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- HY-W142446S
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2,6-Dichlorobenzamide-3,4,5-d3 is the deuterium labeled 2,6-Dichlorobenzamide (HY-W142446). 2,6-Dichlorobenzamide is a herbicide degradation product that is relatively difficult to degrade .
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- HY-113136S
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1-Methylguanosine-d3 (N1-Methylguanosine-d3) is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
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- HY-126534S
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Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
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| Cat. No. |
Product Name |
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Classification |
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- HY-148476
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DBCO
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Tri-GalNAc-DBCO is a synthetic ligand composed of three GalNAc units connected to DBCO. Tri-GalNAc-DBCO can act as a ligand for the sialic acid-degrading protein receptor (ASGPR), and can be coupled with targeting proteins or small molecules to form GalNAc-LYTACs. Tri-GalNAc-DBCO specifically binds to ASGPR and, through receptor-mediated endocytosis, guides the coupled molecules to lysosomes for degradation .
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- HY-147943
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PROTAC Synthesis
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PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-152263
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PROTAC Synthesis
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HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-133138
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Azide
PROTAC Synthesis
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Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) . PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
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- HY-143904
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PROTAC Synthesis
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PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
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- HY-130652
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PROTAC Synthesis
Azide
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Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach . Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-176795
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Alkynes
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SHP2 ligand-3 is a PROTAC target protein ligand that can be used to synthesize SHP2 protein degrader-1 (HY-145159) .
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- HY-W457949
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Azide
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Pomalidomide 4'-alkylC4-azide (Compound 2) is an azide compound containing a MIDI group and is one of the compounds used to construct a library of MIDI azide compounds. Pomalidomide 4'-alkylC4-azide is an E3 ligase ligand and linker conjugate (E3 Ligase Ligand-Linker Conjugate). Pomalidomide 4'-alkylC4-azide can be used to develop research on PROTAC degraders .
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- HY-178035
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Alkynes
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OSBP ligand-1 (Compound 2) is an Oxysterol-binding protein (OSBP) inhibitor. OSBP ligand-1 can be used for synthesis of PROTAC OSBP Degrader-1 (HY-178034) .
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- HY-178118
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Alkynes
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PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation . Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
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- HY-175827
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Alkynes
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MK-5108-NH-PEG2-alkyne is a Aurora kinase A (AURKA) inhibitor. MK-5108-NH-PEG2-alkyne can be used for synthesis of PROTAC AURKA degrader 1 (HY-175830) .
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- HY-159777
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Alkynes
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CPI-203-PEG5-Alkyne is a conjugate of target protein ligase and linker. CPI-203-PEG5-Alkyne can be used for synthesis of PROTAC BRD4-DCAF1 degrader-1 (HY-169151) .
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- HY-163647
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Azide
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Lenalidomide-COCH-PEG2-azido is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based cereblon ligand and a linker. Lenalidomide-COCH-PEG2-azido can be used in the synthesis of PROTAC AKR1C3 degrader-1 (HY-163609) .
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- HY-130984
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PROTAC Synthesis
Azide
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Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-181534
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PROTAC Synthesis
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PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma .
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- HY-181536
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PROTAC Synthesis
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TEAD ligand 2 is a target protein ligand that can be used for the synthesis of PROTACs, such as PROTAC TEAD1/IAP degrader-1 (HY-181534). PROTAC TEAD1/IAP degrader-1 is a potent TEAD1/IAP PROTAC degrader with anti-cancer activity .
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- HY-159452
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Azide
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SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .
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- HY-180901
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Alkynes
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BRD3 ligand-1 is a target protein ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD3 degrader-1 (HY-180889) .
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- HY-180902
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Azide
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Pomalidomide-C11-azide is a synthetic E3 ligase ligand-linker conjugate, which can be used for the synthesis of PROTAC BRD3 degrader-1 (HY-180889) .
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- HY-182978
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PROTAC Synthesis
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Pomalidomide-C3-O-C4-O-C3-NH2 is an E3 ligase ligand-linker conjugate that contains Pomalidomide (HY-10984). Pomalidomide-C3-O-C4-O-C3-NH2 can be used for the synthesis of PROTACs targeting glycogen synthase kinase 3β (GSK-3β), such as PROTAC GSK-3β Degrader-1 (HY-149845) .
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- HY-178067
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Alkynes
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Phthalimidinoglutarimide-5-piperazine-COC2-alkynes is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC BCL-xL/BCL-w Degrader 1 (HY-178066). PROTAC BCL-xL/BCL-w Degrader 1 is a potent BCL-xL/BCL-w PROTAC degrader with anti-cancer activity .
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- HY-179603
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Azide
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E3 Ligase Ligand-linker Conjugate 220 is an E3 ligase ligand-linker conjugate, can be used for synthesis of PROTAC 11β-HSD1 Degrader 1 (HY-179602) .
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