Search Result
Results for "
MG degrader 1
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-128838A
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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-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-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-153880
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PROTACs
Ras
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Cancer
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KRAS degrader-1 (compound 1) is a potent KRAS degrader. KRAS degrader-1 target specific proteins for degradation through the autophagy-lysosomal degradation pathway .
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- HY-W248665A
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Androgen Receptor
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Cancer
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Androgen receptor degrader-1 (compound 18) is a potent androgen receptor degrader. Androgen receptor degrader-1 can be used in research of cancer .
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- HY-163641
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Androgen Receptor
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Cancer
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AR Degrader-1 is an androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR without obvious cytotoxicity in LNCaP prostate cancer cells .
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- HY-145737
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PROTACs
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-156591
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PROTACs
Mixed Lineage Kinase
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Others
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PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax ＞90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
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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-163959
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Others
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Metabolic Disease
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PNPLA3 degrader-1 (Example 11) is a PNPLA3 degrader with an EC50 of 8 nM. PNPLA3 degrader-1 can be used in the study of cirrhosis and hepatocellular carcinoma .
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- HY-145737A
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PROTACs
Ras
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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-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-128845
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PROTACs
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Cancer
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PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader .
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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-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-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-150608
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STING
PROTACs
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Inflammation/Immunology
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PROTAC STING Degrader-1 (Compound SP23) is a STING PROTAC degrader with a DC50 of 3.2 μM. PROTAC STING Degrader-1 shwos anti-inflammatory activity .
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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-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-156401
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Epigenetic Reader Domain
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Cancer
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BRD9 Degrader-1 is a BRD9 degrader. BRD9 Degrader-1 exhibits micromolar binding affinity to BRD9 and nanomolar affinity for the ternary complex with BRD9 and VCB .
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- HY-162014
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PROTACs
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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-162331
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STING
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Inflammation/Immunology
Cancer
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STING Degrader-1 (compound 2) is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 induces STING degradation through a ubiquitin-proteasome system-dependent pathway .
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- HY-156152A
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Histone Methyltransferase
PROTACs
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Cancer
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CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC50 of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration .
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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-158345
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PROTACs
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Cancer
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PROTAC VHL-type degrader-1 (compound 9b) is a VHL-type PROTAC degrader. PROTAC VHL-type degrader-1 induces ATM degradation synergistically enhancing the efficacy of ATR inhibitor AZD6738 .
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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-163295
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ADC Cytotoxin
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-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-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-145071
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PROTACs
Estrogen Receptor/ERR
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Cancer
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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-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-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-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-147654
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PROTACs
Influenza Virus
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Infection
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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-147656
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NAMPT
Autophagy
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Cancer
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NAMPT degrader-1 (Compound A3) 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-161108
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PROTACs
Checkpoint Kinase (Chk)
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Cancer
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PROTAC Chk1 degrader-1 (Compound PROTAC-2 ) is a potent PROTAC-targeted degrader of Chk1 with a DC50 of 1.33 μM. PROTAC Chk1 degrader-1 can be used in cancer research .
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- HY-163372
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MAP4K
PROTACs
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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-D2336
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PROTACs
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Cancer
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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-156244
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PROTACs
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Cancer
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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 .
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- HY-163638
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Molecular Glues
Epigenetic Reader Domain
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Cancer
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BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue BRD4 degrader. BRD4 degrader-1 targets DCAF16 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
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- HY-158045
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PROTACs
PARP
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Inflammation/Immunology
Cancer
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PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
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- HY-168029
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Others
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Cancer
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eEF2K degrader-1 is a type of eEF2K degrader. eEF2K degrader-1 can inhibit the viability, proliferation, and migration of the MDA-MB-231 and HCC1806 cell lines, with an IC50 value of 43.71 nM for MDA-MB-231. eEF2K degrader-1 shows tumor-suppressing effects in mouse models with MDA-MB-231 cell xenografts .
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- HY-128840
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PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase (CN108610333A) .
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- HY-156083
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CDK
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Cancer
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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-163897
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PROTACs
Ferroptosis
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Inflammation/Immunology
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PROTAC NCOA4 degrader-1 (Compound V3) is a PROTAC NCOA4 degrader (DC50: 3 nM in HeLa cells). PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces NCOA4 levels and downregulates intracellular ferrous iron (Fe 2+) levels. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. (Red: NCOA4 ligand (HY-149457). Black: linker (HY-163903). Blue: VHL ligand (HY-138678B)) .
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- HY-146324
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PROTACs
CaMK
Apoptosis
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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-148521
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CDK
FLT3
PROTACs
Apoptosis
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Cancer
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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 .
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- HY-138536
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-149845
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GSK-3
PROTACs
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Neurological Disease
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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 .
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- HY-157764
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PROTACs
ATM/ATR
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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-161749
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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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-147943
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PROTACs
Btk
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Cancer
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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-155816
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PROTACs
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Cancer
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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.
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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-133131
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PROTACs
Epigenetic Reader Domain
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Cancer
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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-168057
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PROTACs
CDK
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Cancer
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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-156152
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Histone Methyltransferase
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Cancer
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PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
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- HY-139186
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PROTACs
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Cancer
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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-130614
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PROTACs
Histone Methyltransferase
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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-155552
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Apoptosis
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Cancer
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GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis .
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- HY-137487
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PROTACs
Raf
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Cancer
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PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value 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). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth .
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- HY-103628
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PROTACs
CDK
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Cancer
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PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
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- HY-155643
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PROTACs
Glutaminase
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Cancer
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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-168037
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PROTACs
PIN1
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Cancer
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PROTAC PIN1 degrader-1 (compound D4) is a PROTAC targeting PIN1, with a DC50=1.8 nM. The GI50 of PROTAC PIN1 degrader-1 to MDA-MB-468 is >30 μM. PROTAC PIN1 degrader-1 is composed of target protein ligand PIN1 ligand-1 (HY-168038) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part), and PROTAC linker (black part) [1] .
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- HY-111844
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SNIPERs
PROTACs
RAR/RXR
|
Cancer
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PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
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- HY-163938
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PROTACs
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Cancer
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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-149678
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PROTACs
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Cancer
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PROTAC eDHFR Degrader-1 is a PROTAC that is effective degradation of eDHFR-YFP, various POIs-including YFP and Luciferase .
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- HY-160525
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Molecular Glues
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Cancer
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CDO1 degrader-1 (compound 8) is a molecular glue degrader that targets cysteine dioxygenase (CDO1) .
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- HY-158985
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AUTACs
Autophagy
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Cancer
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|
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-163757
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PROTACs
PD-1/PD-L1
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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-132998
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PROTACs
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Others
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|
HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation .
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- HY-130709
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PROTACs
CDK
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Cancer
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|
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-115865
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IAP
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Cancer
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|
XIAP degrader-1, a primary amine tethered small molecule, promotes the degradation of X-linked inhibitor of apoptosis protein (XIAP).
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- HY-143904
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PROTACs
|
Cancer
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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-130499
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Target Protein Ligand-Linker Conjugates
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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 .
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- HY-111840
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SNIPERs
PROTACs
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Cancer
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|
PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand .
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-
- HY-155008
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Hexokinase
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Cancer
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|
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-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-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 .
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-
- HY-130612
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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 .
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-
- HY-163609
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PROTACs
Aldose Reductase
|
Cancer
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|
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)) .
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- HY-130620
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PROTAC Linkers
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Cancer
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|
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 .
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-
- HY-131188
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PROTACs
Bcl-2 Family
|
Cancer
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|
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 .
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-
- HY-169008
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PROTACs
Acetyl-CoA Carboxylase
|
Infection
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|
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). (Srtucture Note: Pink, Target protein ligand (HY-169009); Blue, E3 ligand (HY-10984); Black, linker (HY-W007559) .
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-
- HY-163920
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HDAC
|
Cancer
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|
Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells .
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-
- HY-163440
-
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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.
(Srtucture Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
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-
- HY-151110
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PROTACs
CDK
|
Cancer
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|
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 .
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-
- HY-131911
-
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PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
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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 .
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-
- HY-151110A
-
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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 .
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-
- HY-163152
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-
- HY-160262
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-
- HY-168135
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PROTACs
c-Met/HGFR
|
Cancer
|
|
PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models . (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
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-
- HY-162412
-
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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) .
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-
- HY-149236
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-
- HY-158400
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-
- HY-103633
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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.
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-
- HY-W087383
-
-
- HY-160115
-
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Others
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Neurological Disease
|
|
TDP-43 degrader-1 (example 3) reduces the TDP-43 aggregation that can be in the research of Amyotrophic lateral sclerosis and? Alzheimer's disease .
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-
- HY-103636
-
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Sirtuin
PROTACs
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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) .
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-
- HY-157804
-
|
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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 .
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-
- HY-129968
-
|
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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) .
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-
- HY-168191
-
-
- HY-130814
-
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|
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 .
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-
- HY-130819
-
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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) .
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-
- 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 .
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-
- HY-159609
-
|
|
PROTACs
|
Cancer
|
|
PROTAC GSPT1 degrader-1 (Compound F) is a PROTAC degrader for G1 to S phase transition protein 1 (GSPT1) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). PROTAC GSPT1 degrader-1 inhibits the cell viability of HL-60 with an IC50 of 9.2 nM. (Pink: ligand for target protein (HY-W599025); Black: linker (HY-159619); Blue: ligand for E3 ligase (HY-W087383))
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-
- 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) .
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-
- 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-168017
-
-
- 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) .
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-
- HY-161708
-
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|
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))
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-
- HY-130852
-
-
- HY-145479
-
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|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM .
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-
- HY-30105
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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) .
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-
- HY-158678
-
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|
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-138678B
-
-
- HY-125878
-
|
SGK3-PROTAC1
|
PROTACs
SGK
|
Cancer
|
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 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) .
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-
- HY-103632
-
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|
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 .
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-
- 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) .
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-
- HY-158342
-
|
|
PROTACs
YAP
|
Cancer
|
|
PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
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-
- HY-146393
-
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|
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 .
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-
- HY-158679
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-
- 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 .
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-
- 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 .
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-
- 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) .
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-
- 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-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) .
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-
- HY-158142
-
|
|
PROTACs
JAK
|
Cancer
|
|
PROTAC TYK2 degrader-1 (CPD-155) is a PROTAC targeting degrader to TYK2 with Dmax >60%. (Srtucture Note: PINK, TYK2 ligand 1 (HY-158340); Blue, VHL ligand Thalidomide (HY-14658); Black, linker)
|
-
- 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) ) .
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-
- 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-168038
-
-
- 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) .
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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-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) .
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-
- HY-163852
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-
- HY-169152
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-
- 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-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-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-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-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-168016
-
|
|
PROTACs
YAP
|
Cancer
|
|
PROTAC YAP degrader-1 (compound YZ-6) is a PROTAC targeting YAP and also inhibits the nuclear localization of YAP. PROTAC YAP degrader-1 is composed of PROTAC target protein ligand NSC682769 (HY-168017) (red part) and E3 ubiquitin ligase ligand + Linker conjugate (R,S,R)-AHPC-PEG2-C2-boc (HY-168019) (blue+black part), in which the PROTAC Linker used is Acid-PEG2-C2-Boc (HY-140480) and the target protein ligand activity control is Demethyl-NSC682769 (HY-168018) [1] .
|
-
- 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-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-W599025
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
5-Br-4-Cl-Pyrrolo-pyroxypyridine is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). 5-Br-4-Cl-Pyrrolo-pyroxypyridine can be used for synthesis 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-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-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-159777
-
-
- HY-129966
-
|
|
PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively .
|
-
- 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-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-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-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-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-130713
-
-
- HY-168019
-
-
- HY-130707
-
|
|
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-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
-
|
|
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-130815
-
-
- HY-130815A
-
-
- 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 .
|
-
- HY-169151
-
-
- 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-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-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-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-125876
-
|
|
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).
|
-
- HY-130619
-
|
|
PROTAC Linkers
|
Cancer
|
|
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 .
|
-
- HY-131187
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
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 .
|
-
- HY-133138
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-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.
|
-
- HY-130984
-
|
|
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.
|
-
- HY-108369
-
|
|
PROTAC Linkers
|
Cancer
|
|
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.
|
-
- HY-160531
-
|
|
IKZF Family
|
Cancer
|
|
IKZF1-degrader-1 (Compound 9-B) is a degrader to IKZF1 protein, with DC50 value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors .
|
-
- HY-142662
-
|
|
PROTACs
|
Others
|
|
PROTAC IRAK3 degrade-1 (compound 23) is a potent and selective degrader of IRAK3 (IC50 = 5 nM) .
|
-
- HY-144624
-
|
|
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 .
|
-
- HY-142662A
-
|
|
PROTACs
|
Others
|
|
PROTAC IRAK3 degrade-1 (compound 23) formic is a potent and selective degrader of IRAK3 (IC50=5 nM) .
|
-
- HY-162665
-
|
|
Others
|
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 .
|
-
- HY-156747
-
-
- HY-155582
-
|
|
Others
|
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 .
|
-
- HY-159728
-
-
- HY-141482
-
|
|
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 .
|
-
- HY-162282
-
|
|
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 .
|
-
- HY-162318A
-
|
|
c-Myc
|
Cancer
|
|
MYC degrader 1 TFA is a MYC degrader that restores pRB1 protein activity and reduces MYC-dependent CDK4/6 resistance. MYC degrader 1 TFA has antitumor activity .
|
-
- HY-130245A
-
|
|
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 .
|
-
- HY-162960
-
|
|
Ras
|
Cancer
|
|
pan-KRAS degrader 1 (Compound 1) is a panKRAS degrader with a surface plasmon resonance (SPR) dissociation constant Ki value of 25 nM for KRAS G12V .pan-KRAS degrader 1 has antitumor activity .
|
-
- HY-157458
-
|
|
ATTECs
Phosphodiesterase (PDE)
Autophagy
|
Cancer
|
|
PDEδ autophagic degrader 1 (compound 12c) 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-162608
-
|
|
PROTACs
|
Cancer
|
|
PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC50 of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker) .
|
-
- HY-169077
-
|
|
Others
|
Cancer
|
|
IKZF3 degrader 1 (compound 19a) is an IKZF3 degrader (EC50=0.012 μM, 9.2% Ymin). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 .
|
-
- HY-162896
-
|
|
Others
|
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-149917
-
|
|
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). 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 also shows good plasma exposure levels .
|
-
- HY-163814
-
|
|
CDK
|
Cancer
|
|
CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. 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 (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) .
|
-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (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 .
|
-
- HY-163640
-
|
|
CDK
|
Cancer
|
|
CDK4 degrader 1 (ML 1–71) is a monovalent degrader targeting CDK4 .
|
-
- 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-161176
-
|
|
PROTACs
|
Cancer
|
|
PROTAC KRAS G12D degrader 1 is a potent, rapid, and selective degrader of protac KRAS G12D with DC 50 of 38.06 nM. PROTAC KRAS G12D degrader 1 showes significant antitumor efficacy .
|
-
- HY-162307
-
|
|
PROTACs
Keap1-Nrf2
|
Cancer
|
|
Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer effects. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively .
|
-
- HY-159592
-
|
|
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) .
|
-
- HY-152263
-
|
|
PROTACs
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-156745
-
-
- HY-156746
-
-
- HY-161796
-
-
- 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-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-158767
-
|
|
Others
|
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-162318
-
|
|
c-Myc
|
Cancer
|
|
MYC degrader 1 (compound A80.2HCl) is an orally available MYC degrader with antitumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC over-expressing cancer cells to CDK4/6 inhibitors .
|
-
- 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-137343
-
-
- HY-156744
-
-
- HY-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
|
-
- HY-162930
-
|
|
PROTACs
METTL3
|
|
|
PROTAC METTL3 degrader 1 (Compound KH12) 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 has anti-proliferative activities against AML cells. Black: Linker (HY-ER002); Red: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217) .
|
-
- 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-162723
-
|
|
PROTACs
AP-1
|
Cancer
|
|
FOSL1 degrader 1 (4) is a T-5224-PROTAC, potently degrade FOSL1 (AP-1) to suppress cancer stemness gene expression in HNSCC. FOSL1 degrader 1 (4) effectively eliminate HNSCC cancer stem cells to inhibit tumor growth through degrading FOSL1. FOSL1 degrader 1 (4) displays around 30- to 100-fold increased potency over T-5224 (Pink: T-5224 (HY-12270); Black: Linker (HY-130200); Blue: Pomalidomide (HY-10984)) .
|
-
- 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-161168
-
|
|
CDK
|
Cancer
|
|
Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM .
|
-
- 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-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-N8180
-
|
|
Others
|
Others
|
|
Silyamandin is a flavonolignan compound. Silydianin can form Silyamandin through oxidative degradation .
|
-
- HY-153368
-
|
|
IRAK
|
Cancer
|
|
KT-413 (example I-3) is a potent IRAK degrader .
|
-
- 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-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-141551B
-
|
|
Others
|
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-155398
-
-
- HY-155397
-
-
- HY-119932
-
|
|
PROTACs
FAK
|
Cancer
|
|
PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM .
|
-
- 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-150859
-
|
|
HDAC
|
Cancer
|
|
HDAC ligand-1 is a HDAC ligand that can be used to synthesize PROTAC HDAC degraders .
|
-
- HY-157765
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-6 (compound A3) is a potent PROTAC degrader of ERα, with DC50 of 0.12 μM. 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-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-162626
-
|
|
FGFR
|
Cancer
|
|
FGFR2 degrader 1 (compound 28E) is a selectively degrader of FGFR2, with the DC50 of 0.645 nM. FGFR2 plays an important role in cancer research .
|
-
- HY-148523
-
|
|
Others
|
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-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-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-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-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-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-113136
-
|
N1-Methylguanosine
|
Endogenous Metabolite
|
Cancer
|
|
1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
|
-
- HY-W584512
-
|
|
Others
|
Others
|
|
Thalidomide-NH-CH2-COO (t-Bu) is a molecular block of small-molecule degrader .
|
-
- HY-157582
-
|
|
Others
|
Others
|
|
MS39N (compound 27) is a negative control for MS39 that binds EGFR without inducing 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-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-169235
-
-
- HY-114323
-
|
|
PROTACs
FLT3
Apoptosis
|
Cancer
|
|
PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction .
|
-
- 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-143346
-
|
|
Others
|
Cancer
|
|
CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders .
|
-
- HY-150400
-
-
- 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-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 (Srtucture Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
|
-
- 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-163168
-
|
CFT-4531
|
DNA/RNA Synthesis
|
Cancer
|
|
aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki value of 1.8 nM.
degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader .
|
-
- HY-153042
-
-
![Thalidomide-NH-C2-azaspiro[3.5]nonane hydrochloride](//file.medchemexpress.eu/product_pic/hy-153042.gif)
- HY-161597
-
|
|
PROTACs
|
Cancer
|
|
PROTAC DYRK2 degrader 1 (compound CP134) is a PROTAC degrader of DYRK2 (Red: DYRK2 inhibitor(HY-161598), black: linker (HY-42776), Blue: E3 ligase ligand (HY-10984)) .
|
-
- HY-N2057
-
|
|
Aquaporin
|
Metabolic Disease
|
|
Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- HY-139340
-
|
|
Others
|
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-133017
-
|
SAR439859
|
Estrogen Receptor/ERR
|
Cancer
|
|
SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation . SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER + breast cancer .
|
-
- HY-163786
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
|
-
- HY-120722
-
TCH-165
1 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-130640
-
-
- HY-118653
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation .
|
-
- HY-W017389
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-161575
-
-
- HY-161598
-
-
- 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-169094
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
PFI-6-COOH (Compound 18) is an eleven-nineteen leukemia (ENL) ligand, and can be used for synthesis of MS41 (HY-169093), an ENL PROTAC degrader .
|
-
- HY-162973
-
-
- 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-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-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-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-113136S
-
|
N1-Methylguanosine-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Others
|
|
1-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-160438
-
|
|
Others
|
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-160438A
-
|
|
Others
|
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-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-169158
-
-
- 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-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-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-157592
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
|
-
- HY-129363
-
-
- HY-161746
-
|
|
AUTOTACs
Autophagy
|
Cancer
|
|
Anle138b-F105 is an autophagy targeting chimera (AUTOTAC) with DC50 values of 3 nM. Anle138b-F105 targetes tauP301L for lysosomal degradation .
|
-
- HY-N2057R
-
|
|
Aquaporin
|
Metabolic Disease
|
|
Steviol (Standard) is the analytical standard of Steviol. This product is intended for research and analytical applications. Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- 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-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-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[1][2].
|
-
- HY-N7045
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) 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-156395
-
|
|
Others
|
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-D2259
-
|
|
E1/E2/E3 Enzyme
|
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-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-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-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-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-126534
-
-
- 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-130800
-
-
- HY-157591
-
|
|
Others
|
Others
|
|
MMH1-NR, containing a non-reactive (ethyl) group is a negative control of MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
|
-
- HY-W003696
-
|
Tert-butyl 5-bromo-1,3-dihydro-2H-isoindole-2- carboxylate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 5-bromoisoindoline-2-carboxylate is a PROTAC Linker. tert-Butyl 5-bromoisoindoline-2-carboxylate can be used in synthesis PTOTAC HSD17B13 degrader 1 (HY-159651) .
|
-
- 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-W017389R
-
|
|
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-130648
-
-
- HY-162411
-
|
|
Others
|
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-13822
-
SKI II
4 Publications Verification
|
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-163986
-
-
- 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-122725B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .
|
-
- HY-122725A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .
|
-
- HY-137342
-
|
|
PROTACs
|
Cancer
|
|
SB1-G-187, a PROTAC, is a multi-kinase degrader . SB1-G-187 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-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-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-13982
-
JSH-23
Maximum Cited Publications
91 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-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-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-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-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-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-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-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-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-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-125001
-
|
|
Others
|
Others
|
|
JH-VIII-49 is a potent and selective CDK8 inhibitor with excellent biological activity. The synthesis of JH-VIII-49 is simplified to eight steps with an overall yield of 33%, making it suitable for large-scale production. JH-VIII-49 promotes CDK8 inhibition through its steroid skeleton design. JH-VIII-49 provides a basis for the subsequent development of more complex bivalent small molecule degraders .
|
-
- 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.
|
-
- HY-151792
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
|
-
- 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-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-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-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-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 .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D2336
-
|
|
Fluorescent Dyes/Probes
|
|
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/Probes
|
|
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 |
Target |
Research Area |
-
- HY-169235
-
-
- HY-P2191
-
|
|
Peptides
|
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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-126534S
-
|
|
|
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[1][2].
|
-
-
- HY-113136S
-
|
|
|
1-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-W017389S
-
|
|
|
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 .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-133138
-
|
|
|
Azide
|
|
Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-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.
|
-
- HY-108369
-
|
|
|
PROTAC Synthesis
Azide
|
|
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.
|
-
- HY-130652
-
|
|
|
Azide
|
|
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.
|
-
- HY-159777
-
|
|
|
Alkynes
|
|
CPI-203-PEG5-Alkyne is a conjugate of E3 ligase and linker. CPI-203-PEG5-Alkyne can be used for synthesis of PROTAC BRD4-DCAF1 degrader-1 (HY-169151) .
|
-
- HY-163647
-
|
|
|
Azide
|
|
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-130984
-
|
|
|
PROTAC Synthesis
Azide
|
|
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.
|
-
- HY-159452
-
|
|
|
Azide
|
|
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-W457949
-
|
|
|
Azide
|
|
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 can be used to develop research on PROTAC degraders .
|
-
- HY-151792
-
|
|
|
PROTAC Synthesis
Azide
|
|
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
|
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