Search Result
Results for "
Ubiquitin ligase
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156382
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Akt
ERK
E1/E2/E3 Enzyme
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Cancer
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SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. SPOP-IN-1 leads to the accumulation of tumor suppressors PTEN and DUSP7 and decreased levels of phosphorylated AKT and ERK in clear-cell renal cell carcinoma .
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- HY-143715
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Ligands for E3 Ligase
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Cancer
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Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
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- HY-W595340
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Ligands for E3 Ligase
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Cancer
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E3 ubiquitin ligase binder-1 (compound 11) is a potent E3 ubiquitin ligase binder. E3 ubiquitin ligase binder-1 is a ligand for E3 Ligase .
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- HY-18327
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E1/E2/E3 Enzyme
MDM-2/p53
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Cancer
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HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation .
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- HY-49514
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Ligands for E3 Ligase
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Cancer
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VHL Ligand intermediate-1 (intermediate 18a) is an intermediate in the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .
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- HY-49515
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Ligands for E3 Ligase
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Cancer
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VHL Ligand intermediate-2 (compound 18c) is an intermediate for the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .
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- HY-W145436
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- HY-169968
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Ligands for E3 Ligase
E1/E2/E3 Enzyme
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Cancer
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E3 ligase Ligand 41 (Compound SI-13) is a ligand for E3 ubiquitin ligase DCAF16. E3 ligase Ligand 41 can be connected to SLF (HY-114872) by a linker (HY-W040168) to form KB03-SLF (HY-147196) .
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- HY-168316
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- HY-169969
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- HY-169390
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Ligands for E3 Ligase
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Cancer
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OICR-8268-acrylic acid is a ligand for E3 ubiquitin ligase. OICR-8268-acrylic acid can be connected to the ligand for protein by a linker to form OICR41114 (HY-169389). OICR41114 can be used in anti-cancer research .
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- HY-10949
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E1/E2/E3 Enzyme
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Cancer
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SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF) Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF Met30 .
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- HY-44432
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ABT-263-piperazine
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Bcl-2 Family
Ligands for Target Protein for PROTAC
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Cancer
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Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor. Navitoclax-piperazine and a VHL ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC DT2216 (HY-130604) with anti-tumor activity .
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- HY-169325
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Molecular Glues
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Cancer
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(S)-ACE-OH is a molecular glue with anticancer activity. (S)-ACE-OH promotes nucleoporin degradation and disruption of nucleocytoplasmic trafficking by inducing the interaction between E3 ubiquitin ligase TRIM21 and nucleoporin NUP98 .
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- HY-49444
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NF-κB
Molecular Glues
E1/E2/E3 Enzyme
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Cancer
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EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
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- HY-W062696
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E1/E2/E3 Enzyme
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Inflammation/Immunology
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BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity .
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- HY-168304
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(R)-Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 is the E3 ubiquitin ligase ligand and linker of PROTAC (R)-NX-2127 (HY-153220A), which can be used in cancer research .
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- HY-168690
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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6-Aminocaproic acid-(S,R,S)-AHPC-Me is a ligand and linker for the E3 ubiquitin ligase of PROTAC, which can be used to synthesize PVD-06 (HY-149760) and is used in tumor research .
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- HY-43722
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Ligands for E3 Ligase
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Cancer
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Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602) .
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- HY-134417
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NSC2805
1 Publications Verification
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Others
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Cancer
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NSC2805 is a WWP2 ubiquitin ligase inhibitor that can significant inhibit WWP2 activity with an IC50 of 0.38 μM. NSC2805 can be used for the research of cancer .
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- HY-130815
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- HY-130815A
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- HY-108640A
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MDM-2/p53
Parasite
Apoptosis
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Infection
Cancer
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HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents . Antimalarial activity .
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- HY-108640
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MDM-2/p53
Parasite
Apoptosis
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Infection
Cancer
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HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents . Antimalarial activity .
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- HY-W877989
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Ligands for E3 Ligase
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Cancer
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BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 .
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- HY-123967
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E1/E2/E3 Enzyme
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Inflammation/Immunology
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RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research .
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- HY-128756
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PROTACs
Bcr-Abl
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Cancer
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SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity .
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- HY-130683
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-propargyl-C2-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Lenalidomide-propargyl-C2-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312) . Lenalidomide-propargyl-C2-NH2 (hydrochloride) 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-130682
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312) . Lenalidomide-propargyl-C2-amido-Ph-NH2 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-153424
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Target Protein Ligand-Linker Conjugates
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Cancer
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PROTAC SMARCA2 degrader-1 (compound ex7) is a BRM2 (SMARCA2) degrader (DC50<0.1 μM). PROTAC SMARCA2 degrader-1 is also an E3 ubiquitin ligase binding linker useful in research of cancers. PROTAC SMARCA2 degrader-1 is a target protein ligand-linker conjugate .
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- HY-133046
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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.
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- HY-168290
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide can be used in the synthesis of PROTACs, such as MS934 (HY-153863). MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader .
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- HY-153357
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PROTACs
Btk
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Cancer
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NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM) . NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 can bind non-covalently to the BTK binding domain and cereblon, which is an adapter protein in the E3 ubiquitin ligase complex . NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263). E3 ubiquitin ligase and linker can form Thalidomide 5-pyrrolidine-CHO (HY-49372A); the active control for the target protein ligand is BTK ligand 12 (HY-49421).
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- HY-47879
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Others
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Others
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WAY-304671 is an active molecule and a potential ubiquitin ligase inhibitor.
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- HY-156499
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Others
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Others
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RNF114 ligand 1 is a E3 Ubiquitin ligase binder .
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- HY-162855
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 33 (56-9B) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 33 can be used in anti-cancer research .
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- HY-401613
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 43 serves as the E3 ubiquitin ligase ligand for ACBI3 (HY-157228). E3 ligase Ligand 43 can be utilized for the synthesis of PROTACs .
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- HY-157589
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- HY-162188
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- HY-162201
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- HY-168253
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- HY-169995
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- HY-120204
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BI8626
1 Publications Verification
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E1/E2/E3 Enzyme
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Cancer
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BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM .
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- HY-120929
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BI8622
3 Publications Verification
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E1/E2/E3 Enzyme
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Cancer
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BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM .
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- HY-W454906
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Ligands for E3 Ligase
Autophagy
Apoptosis
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Cancer
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tDHU, acid is a dihydropyrimidinecereblon ligand that contains an E3 ligase ligand and a benzoic acid linker. tDHU, acid can be used as an E3 ubiquitin ligase ligand-Linker conjugate for the development of PROTACs .
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- HY-159733
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- HY-169990
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- HY-128807
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-129653
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-128811
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-43961
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-128810
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-165161
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HIV
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Infection
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POSH-IN-1 (Compound 108) is an inhibitor for POSH polypeptide, that inhibits the ubiquitin ligase of POSH with an IC50 of 900 nM .
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- HY-170305
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- HY-169979
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- HY-128806
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
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- HY-144980
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
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- HY-144983
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
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- HY-142621
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PROTACs
Btk
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Cancer
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BCPyr is a PROTAC-class BTK degrader (DC50 = 800 nM) . BCPyr consists of a PROTAC target protein ligand (red part) BTK ligand 11 (HY-168314), an E3 ubiquitin ligase ligand (blue part) E3 ligase Ligand 20 (HY-135997), and a PROTAC linker (black part) (5-(Bromomethyl)pyrazin-2-yl)methanol (HY-168315). E3 ubiquitin ligase+linker can form E3 Ligase Ligand-linker Conjugate 146 (HY-168316).
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- HY-144985
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
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- HY-W797383
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- HY-161185
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Ligands for E3 Ligase
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Cancer
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Thalidomide-piperidine-O-azetidine-boc is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
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- HY-131667
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MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy .
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- HY-146237
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CC-99282
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Ligands for E3 Ligase
Molecular Glues
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Cancer
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Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) .
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- HY-130270
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E3 ligase Ligand-Linker Conjugates 57
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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AhR Ligand-Linker Conjugates 1 (E3 Ligase Ligand-Linker Conjugates 57) incorporates an IAP ligand for the E3 ubiquitin ligase, and a SNIPER linker. AhR Ligand-Linker Conjugates 1 can be used to design SNIPER .
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- HY-49372A
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- HY-W382038
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 32 (First product in Example 52) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 32 can be connected to the ligand for protein by a linker to form PROTACs and can be used for the synthesis of PROTAC SMARCA2/4-degrader-29 (HY-162743) .
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- HY-W1003189
-
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 42 is an E3 ubiquitin ligase ligand. E3 ligase Ligand 42 can be connected to the target protein ligand through a linker and can be used to synthesize PROTAC AR Degrader-6 (HY-156751). PROTAC can induce ubiquitination degradation of cancer-promoting proteins .
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- HY-143346
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- HY-W584512
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- HY-139336
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- HY-125906
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E3 ligase Ligand-Linker Conjugates 56
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs .
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- HY-144841
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CFT7455
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Molecular Glues
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Cancer
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Cemsidomide (CFT7455) is a ubiquitin ligase pathway Ikaros/Aiolos degrader with molecular glue activity . Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells.
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- HY-168349
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- HY-159651
-
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PROTACs
17β-HSD
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Cancer
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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] .
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- HY-132288
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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 .
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- HY-148130A
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RG6091 sodium; RO7248824 sodium
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E1/E2/E3 Enzyme
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Others
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Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
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- HY-129395
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CC-92480
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E1/E2/E3 Enzyme
Molecular Glues
Apoptosis
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Cancer
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Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating agent (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity .
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- HY-W598456
-
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Others
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Cancer
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Brigimadlin intermediate-1 is an intermediate of the E3 ubiquitin protein ligase MDM-2 inhibitor Brigimadlin (HY-152859) and can be used to synthesize Antibody-Drug Conjugates (ADCs) .
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- HY-163219
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- HY-A0003
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Lenalidomide
Maximum Cited Publications
40 Publications Verification
CC-5013
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Inflammation/Immunology
Cancer
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Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-A0003B
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CC-5013 hemihydrate
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Cancer
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Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-A0003A
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CC-5013 hydrochloride
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Ligands for E3 Ligase
Molecular Glues
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Inflammation/Immunology
Cancer
|
|
Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
|
-
- 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-131863
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-alkylC8-acid is an E3 ubiquitin ligase ligand-Linker conjugate containing Pomalidomide (HY-10984). Pomalidomide is a third-generation immunomodulator that acts like a molecular glue. Pomalidomide interacts with the E3 ligase cereblon to induce degradation of the essential Ikaros transcription factor .
|
-
- HY-128813A
-
|
E3 ligase Ligand-Linker Conjugates 34 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs .
|
-
- HY-128815
-
|
E3 ligase Ligand-Linker Conjugates 36
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 14 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 14 can be used to design SNIPERs .
|
-
- HY-128820
-
|
E3 ligase Ligand-Linker Conjugates 41
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 1 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 1 can be used to design SNIPERs .
|
-
- HY-128819
-
|
E3 ligase Ligand-Linker Conjugates 40
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 3 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 3 can be used to design SNIPERs .
|
-
- HY-128812A
-
|
E3 ligase Ligand-Linker Conjugates 33 Hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 11 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 Hydrochloride can be used to design SNIPERs .
|
-
- HY-128813
-
|
E3 ligase Ligand-Linker Conjugates 34
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 15 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 can be used to design SNIPERs .
|
-
- HY-128812
-
|
E3 ligase Ligand-Linker Conjugates 33
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 11 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 can be used to design SNIPERs .
|
-
- HY-128817
-
|
E3 ligase Ligand-Linker Conjugates 38
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 12 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 12 can be used to design SNIPERs .
|
-
- HY-128818
-
|
E3 ligase Ligand-Linker Conjugates 39
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 5 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 5 can be used to design SNIPERs .
|
-
- HY-128816
-
|
E3 ligase Ligand-Linker Conjugates 37
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 2 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 can be used to design SNIPERs .
|
-
- HY-128822
-
|
E3 ligase Ligand-Linker Conjugates 43
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 13 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 13 can be used to design SNIPERs .
|
-
- HY-128816A
-
|
E3 ligase Ligand-Linker Conjugates 37 Hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 2 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 Hydrochloride can be used to design SNIPERs .
|
-
- HY-128826
-
|
E3 ligase Ligand-Linker Conjugates 47
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 10 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 10 can be used to design SNIPERs .
|
-
- HY-128824
-
|
E3 ligase Ligand-Linker Conjugates 45
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 9 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 9 can be used to design SNIPERs .
|
-
- HY-128825
-
|
E3 ligase Ligand-Linker Conjugates 46
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 8 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 8 can be used to design SNIPERs .
|
-
- HY-128823
-
|
E3 ligase Ligand-Linker Conjugates 44
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 7 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 7 can be used to design SNIPERs .
|
-
- HY-128821
-
|
E3 ligase Ligand-Linker Conjugates 42
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 4 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 4 can be used to design SNIPERs .
|
-
- HY-128814
-
|
E3 ligase Ligand-Linker Conjugates 35 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 6 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 6 hydrochloride can be used to design SNIPERs .
|
-
- HY-157435
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumor effect .
|
-
- HY-169989
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
CRBN ligand-11 is the E3 ubiquitin ligase ligand for CFT8634 (HY-145925B). CRBN ligand-11 can be used for the synthesis of PROTACs .
|
-
- HY-111879
-
|
|
SNIPERs
|
Cancer
|
|
Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase .
|
-
- HY-123937
-
|
|
PROTACs
CDK
|
Cancer
|
|
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN) .
|
-
- HY-163222
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
4-Methylanisole-dihydrouracil-imidazo[1,2-a]pyridine-piperidine-NH-Boc is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
|
-
![4-Methylanisole-dihydrouracil-imidazo[1,2-a]pyridine-piperidine-NH-Boc](//file.medchemexpress.com/product_pic/hy-163222.gif)
- HY-163235
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Phenyl phenylcarbamate-CH-5-methoxypicolinamide-CH-CH-Ph-CF3 is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
|
-
- HY-148130
-
|
RG6091; RO7248824
|
E1/E2/E3 Enzyme
|
Others
|
|
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
|
-
- HY-148173
-
-
- HY-168602
-
-
- HY-111878
-
|
|
SNIPERs
|
Cancer
|
|
BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase .
|
-
- HY-169959
-
-
- HY-N0170
-
-
- HY-168312
-
-
![Thalidomide-NH-C2-2-azaspiro[3.3]heptane](//file.medchemexpress.com/product_pic/hy-168312.gif)
- HY-A0003S
-
|
CC-5013-d5
|
Isotope-Labeled Compounds
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
|
-
- HY-130604
-
DT2216
1 Publications Verification
|
Bcl-2 Family
PROTACs
Apoptosis
|
Cancer
|
|
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .
|
-
- HY-130715
-
|
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. 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-135844
-
LS-102
2 Publications Verification
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment .
|
-
- HY-136163
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C2-NH2 dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-OH can be used in the synthesis of a series of PROTACs .
|
-
- HY-131232
-
|
Desmorpholinyl ABT-263-NH-Me
|
Bcl-2 Family
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557) .
|
-
- HY-129773
-
|
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS can be used in the synthesis of a series of PROTACs. 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-129774
-
|
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH can be used in the synthesis of a series of PROTACs. 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-A0003R
-
|
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
|
-
- HY-128843
-
|
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .
|
-
- HY-128842
-
|
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .
|
-
- HY-110204
-
Heclin
2 Publications Verification
|
E1/E2/E3 Enzyme
Akt
MyD88
|
Others
|
|
Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC50 values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer .
|
-
- HY-148671
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-amido-C7-acid incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design PROTACs .
|
-
- HY-151227
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VL285 Phenol is a phenol-based VL285 analog. VL285 is an E3 ubiquitin ligase VHL ligand and can be used in the synthesis of HaloPROTAC3, degrading HaloTag7 fusion protein (IC50=0.34 μM).
|
-
- HY-168310
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-C-Pip is a conjugate of E3 ubiquitin ligase ligand + Linker, used for the synthesis of PROTAC FHD-609 (HY-153367) .
|
-
![(S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-C-Pip](//file.medchemexpress.com/product_pic/hy-168310.gif)
- HY-157228
-
|
|
PROTACs
Others
|
Cancer
|
|
ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995) .
|
-
- HY-133144
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137) .
|
-
- HY-130988A
-
|
GDC-0068-NH2 dihydrochloride; RG7440-NH2 dihydrochloride
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase .
|
-
- HY-149316
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension .
|
-
- HY-A0003S2
-
|
CC-5013-13C5,15N
|
Ligands for E3 Ligase
Apoptosis
Molecular Glues
Isotope-Labeled Compounds
|
Inflammation/Immunology
Cancer
|
|
Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
|
-
- HY-149452
-
|
|
Androgen Receptor
|
Cancer
|
|
SJ1008066 is a MAGE-A11 inhibitor with anIC50 of 0.13 μM. SJ 1008066 binds to the MAGE homology domain (MHD) and disrupts MAGE-A11:PCF11 interaction .
|
-
- HY-136160
-
|
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride can be used to design the PROTACs .
|
-
- HY-128841
-
|
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase (CN108610333A) .
|
-
- HY-144841A
-
|
(Rac)-CFT7455
|
Molecular Glues
|
Cancer
|
|
(Rac)-Cemsidomide ((Rac)-CFT7455) is the racemate of Cemsidomide (HY-144841) with antitumor activity . Cemsidomide is a ubiquitin ligase pathway Ikaros/Aiolos degrader with molecular glue activity. Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells.
|
-
- HY-152859
-
|
BI 907828
|
E1/E2/E3 Enzyme
MDM-2/p53
|
Cancer
|
|
Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research .
|
-
- HY-157512
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
SJF-0661 is a variant of the von Hippel-Lindau (VHL) protein ligand with no targeted degradation ability and can be used as a control reagent for the VHL ubiquitin ligase ligand. SJF-0661 is a variant obtained by inverting the stereocenter of the key hydroxyproline group in the VHL ligand .
|
-
- HY-163218
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
|
-
- HY-131318
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609) .
|
-
- HY-163214
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S)-PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.
|
-
- HY-155075
-
|
|
PROTACs
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
NC-R17 is a PROTAC-class, non-covalent GPX4 degrader based on RSL3, involved in ferroptosis. NC-R17 has antitumor activity and is used for non-covalent GPX4 PROTAC design . NC-R17 consists of a target protein ligand (red part) Demethyl-RSL3 (HY-135832); an E3 ubiquitin ligase ligand (blue part) Lenalidomide (HY-A0003) and a PROTAC linker (black part) (HY-169376). E3 ubiquitin ligase and linker can form Lenalidomide-C13-piperazine-Boc (HY-169377) .
|
-
- HY-159579
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
CW-3308 is an orally effective PROTAC that selectively targets BRD9 and is expected to be used to inhibit synovial sarcoma, rhabdomyoma, and other BRD9-dependent human diseases. CW-3308 is composed of PROTAC target protein ligand Naphthyridin-Me-dimethoxybenzene-COOH (HY-159596) (red part), Linker 3-Azaspiro[5.5]undecane-9-methanol (HY-159598) (black part), E3 ubiquitin ligase ligand Thalidomide-methylpyrrolidine (HY-159597) (blue part), where the conjugate of E3 ubiquitin ligase ligand + linker is Thalidomide-pyrrolidine-C-azaspiro (HY-159599) [1] .
|
-
- HY-159608
-
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|
PROTACs
|
Cancer
|
|
PROTAC Cbl-b-IN-1 (compound 64) is a PROTAC targeting Cbl-b. PROTAC Cbl-b-IN-1 is composed of PROTAC target protein ligand Cbl-b-IN-21 (HY-159615), PROTAC Linker Cbz-Pip-2C-Pip-C-Pip (HY-159617) and E3 ubiquitin ligase ligand (3S) Lenalidomide-5-Br (HY-W797329), where the E3 ubiquitin ligase ligand + Linker conjugate is (3S) Lenalidomide-5-Pip-C-Pip-2C-Pip (HY-159618) [1] .
|
-
- HY-122702
-
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|
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-130835
-
|
RC32
|
PROTACs
FKBP
|
Cancer
|
|
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984) .
|
-
- HY-141651
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-COOH (compound 28i) is a carboxylic acid derivative of the VHL E3 ubiquitin ligase ligand-Linker conjugate. (S,R,S)-AHPC-C3-COOH can be used to synthesize PROTACs .
|
-
- HY-69220
-
|
|
PROTAC Linkers
|
Cancer
|
|
7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. 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 . 7-Octynoic acid 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-129772
-
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|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. 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-40178
-
|
|
PROTAC Linkers
|
Cancer
|
|
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. 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-137341
-
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|
PROTACs
|
Cancer
|
|
SK-3-91 is a PROTAC-type multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases) . SK-3-91 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) TAE648 (HY-169396), the E3 ubiquitin ligase ligand (blue part) Thalidomide-NH-CH2-COOH (HY-131717) and the PROTAC linker (Bromo-PEG1-C2-azide) (HY-140819). The E3 ligase ligand and linker can form a conjugate (HY-169397).
|
-
- HY-162281
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC SOS1 degrader-6 (compound 23) is an effective SOS1 PROTACs degrader that synergizes with KRAS G12C inhibitors . PROTAC SOS1 degrader-6 consists of the target protein ligand (red part) SOS1 Ligand intermediate-7 (HY-169371), E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and PROTAC linker (black part) 5-Bromopentanoic acid (HY-W016456). Among them, the E3 ubiquitin ligase ligand + linker can form (S,R,S)-AHPC-CO-C4-bromine (HY-169372).
|
-
- HY-163962
-
|
|
PROTACs
Btk
|
Inflammation/Immunology
|
|
L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964) [1] .
|
-
- HY-130798
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180) .
|
-
- HY-132992
-
-
- HY-160221
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC50 value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305) .
|
-
- HY-130618
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH can be used in the synthesis of a series of PROTACs. 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-112811
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC .
|
-
- HY-14658
-
|
|
Ligands for E3 Ligase
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
|
-
- 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-113921
-
|
|
PROTAC Linkers
|
Cancer
|
|
m-PEG4-propargyl is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG4-propargyl 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-114670
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG4-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG4-amine 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-115414
-
|
|
PROTAC Linkers
|
Cancer
|
|
Bis-propargyl-PEG8 (compound 16e) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-propargyl-PEG8 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-117045
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG12-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG12-OH 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-130147
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG5-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG5-OH 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-121507
-
|
|
PROTAC Linkers
|
Cancer
|
|
Hydroxy-PEG2-C2-sulfonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-130390
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG4-O-C1-NHS ester (compound 8) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG4-O-C1-NHS ester 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-130554
-
|
|
PROTAC Linkers
|
Cancer
|
|
m-PEG9-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-130137
-
|
|
PROTAC Linkers
|
Cancer
|
|
m-PEG8-C10-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-130373
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG9-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG9-amine 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-133230
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG10-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG10-amine 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-130378
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG7-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG7-alcohol 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-130382
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG6-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG6-alcohol 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-133229
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG4-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG4-alcohol 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-126977
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG9-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG9-OH 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-130374
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG8-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG8-OH 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-130375
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG7-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG8-Boc 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-130380
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG7-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG7-Boc 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-130384
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG6-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG6-Boc 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-130146
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG3-phosphonic acid diethyl ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG3-phosphonic acid diethyl ester 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-130389
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG4-O-C1-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG4-O-C1-Boc 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-130563
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG3-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG3-CH2COOH 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-130584
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG2-MS is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG2-MS 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-133049
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG3-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . Propargyl-PEG3-phosphonic acid 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-130819
-
|
|
PROTAC Linkers
|
Cancer
|
|
Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .
|
-
- HY-112559
-
|
|
PROTAC Linkers
|
Cancer
|
|
Bis-PEG2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-120587
-
|
|
PROTAC Linkers
|
Cancer
|
|
Bis-PEG6-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-126891
-
|
|
PROTAC Linkers
|
Cancer
|
|
Bis-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-140015
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs . TCO-PEG3-acid is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
|
-
- HY-141159
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141160
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG6-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141161
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141162
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG12-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141166
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG3-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141168
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG6-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141169
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG8-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141177
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141178
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG3-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141179
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG4-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141180
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG6-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141181
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG8-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141183
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG4-biotin is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141187
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG3-TCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141188
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG4-TCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-141189
-
|
|
PROTAC Linkers
|
Cancer
|
|
TCO-PEG8-TCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
|
-
- HY-117100
-
|
|
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG14-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG14-OH 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-129610
-
|
|
PROTACs
FKBP
|
Cancer
|
|
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF .
|
-
- HY-137340
-
|
|
PROTACs
|
Cancer
|
|
WH-10417-099 is a CRBN-type PROTAC multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). WH-10417-099 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway and consists of the target protein ligand (red part) PI3Kγ ligand 1 (HY-168319), the E3 ubiquitin ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547) and the PROTAC linker (black part) Amino-PEG5-C2-acid (HY-115384). The E3 ligase ligand and linker can form a conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
|
-
- HY-156730
-
|
|
Molecular Glues
STAT
|
Cancer
|
|
KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
|
-
- HY-14658S
-
-
- HY-145898
-
|
14-D-Valine-TPL
|
c-Myc
Molecular Glues
|
Cancer
|
|
WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .
|
-
- HY-162250
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .
|
-
- HY-157510
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .
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- HY-157511
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-O-C5-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C5-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C5-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .
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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-130713
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-
- HY-123844
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dBET57
3 Publications Verification
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4 Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1 .
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- HY-156106
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Ligands for E3 Ligase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .
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- HY-156730B
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Molecular Glues
STAT
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Cancer
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KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
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- HY-150797
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QA-68-ZU81
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PROTACs
Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).
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- HY-153368
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KT-413
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IRAK
PROTACs
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Cancer
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KT-413 (example I-3) is an orally active PROTAC-class IRAK degrader . KT-413 consists of a target protein ligand (red part) PROTAC IRAK4 ligand-5 (HY-168311), an E3 ubiquitin ligase ligand (blue part) Thalidomide-4-Br (HY-W039116), and a PROTAC linker (black part) 2-(2-Azaspiro[3.3]heptan-6-yl)ethanamine (HY-168313). E3 ubiquitin ligase and linker can form Thalidomide-NH-C2-2-azaspiro[3.3]heptane (HY-168312). The active control for the target protein ligand is RSL3-4-Me (HY-169375).
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- HY-161989
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PROTACs
BCL6
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Cancer
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DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949) [1] .
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- HY-168026
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PROTACs
Mixed Lineage Kinase
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Cancer
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CEP1347-VHL-02 is a PROTAC targeting MLK3. CEP1347-VHL-02 consists of PROTAC target protein ligand CEP-1347 (HY-10412) (red part), E3 ubiquitin ligase ligand (S,R,S)-AHPC-Me (HY-112078) (blue part) and PROTAC Linker Amino-PEG3-CH2COOH (HY-140189) (black part), of which the target protein ligand activity control is CEP-1347-acid (HY-168027), and the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 (HY-131387) [1] .
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- HY-157515
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide 4'-ether-PEG2-azide is a click chemistry modified cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide 4'-ether-PEG2-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkynyl groups. Thalidomide 4'-ether-PEG2-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .
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- HY-169072
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PROTACs
Mixed Lineage Kinase
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Cancer
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PROTAC MLKL Degrader-2 (compound MP-1) is a PROTAC targeting MLKL (Mixed Lineage Kinase). PROTAC MLKL Degrader-2 is composed of PROTAC target protein ligand PROTAC MLKL Degrader-2 (HY-169072) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part) and PROTAC Linker N-Methylpiperazine (HY-78871) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-N-methylpiperazine (HY-169074) [1] .
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- HY-168274
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PROTACs
Apoptosis
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Cancer
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|
PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .
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- HY-136008A
-
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VH032-PEG1-NH2 dihydrochloride
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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(S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-PEG1-NH2 dihydrochloride can be used to design PROTACs .
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- HY-131385
-
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Ligands for E3 Ligase
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Cancer
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KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610) .
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- HY-155269
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-5-C13-NH2 hydrochloride is a Pomalidomide (HY-10984)-based E3 ubiquitin ligase cereblon (CRBN) ligand for recruiting cereblon proteins. Pomalidomide-5-C13-NH2 hydrochloride can be connected to protein ligands through a linker to form PROTAC.
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- HY-161828
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PROTACs
CDK
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Cancer
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JWZ-5-13 is a potent CDK7 PROTAC degrader that significantly degrades CDK7 via the ubiquitin-proteasome system. JWZ-5-13 has antitumor activity. (Pink: Target protein ligand (HY-161830); Black: linker (HY-Y0925); Blue: E3 ligase ligand (HY-112078)) .
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- HY-162809
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Ras
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Cancer
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XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used in cancer research .
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- HY-130619
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PROTAC Linkers
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Cancer
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Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins .
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- HY-156730A
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Molecular Glues
STAT
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Cancer
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KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
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- HY-130988
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GDC-0068-NH2; RG7440-NH2
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Ligands for Target Protein for PROTAC
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Cancer
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|
Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase .
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- HY-163210
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Ligands for E3 Ligase
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Cancer
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|
Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride (ZJT1) is an E3 ubiquitin ligase cereblon based on Pomalidomide (HY-10984) (CRBN) ligand for recruitment of cereblon protein. Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride can be linked to protein ligand by linker to form PROTAC .
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- HY-130816
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VH032-O-Ph-PEG1-NH2
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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|
(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-129917
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PROTACs
Epigenetic Reader Domain
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Cancer
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|
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
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- HY-149760
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PROTACs
Phosphatase
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Cancer
|
|
PVD-06 is a selective PROTAC-class PTPN2 degrader (PTPN2/PTP1B selectivity index >60-fold) with anticancer activity. PVD-06 induces PTPN2 degradation via ubiquitination and proteasome-dependent pathways. PVD-06 can promote T cell activation and amplify IFN-γ-mediated cytotoxicity . PVD-06 consists of a target protein ligand (red part) PTPN2 ligand 1 (HY-168691), a PROTAC linker (black part) 6-Aminocaproic acid (HY-B0236), and an E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC-Me (HY-112078). E3 ubiquitin ligase+linker can form 6-Aminocaproic acid-(S,R,S)-AHPC-Me (HY-168690).
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- HY-157213
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Apoptosis
PROTACs
FLT3
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Cancer
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LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
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- HY-161958
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PROTACs
Histone Acetyltransferase
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Cancer
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|
dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961) [1] .
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-
- HY-108374
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PROTAC Linkers
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Cancer
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|
4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. 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 . 4-Azidobutylamine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-14658R
-
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Ligands for E3 Ligase
Autophagy
Apoptosis
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Inflammation/Immunology
Cancer
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|
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
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- HY-159973
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Ligands for E3 Ligase
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Cancer
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|
Me-SJ46411 is an E3 ubiquitin ligase ligand, which can be used for the synthesis of PROTAC molecules. For example, Me-SJ46411 combined with PROTAC linker Boc-Piperazine-OH (HY-20797) and target protein ligand (+)-JQ-1 (HY-13030) can be used to synthesize the selective BRD3 PROTAC degrader SJ46420 (HY-168635). .
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-
- HY-169358
-
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PROTACs
Epigenetic Reader Domain
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Cancer
|
|
L134 is a potent PROTAC BRD4 degrader with a DC50 value of 7.36 nM. L134 mediates the degradation of BRD4 via the ubiquitin-proteasome system in a DCAF11-dependent manner (Blue: JQ-1 (carboxylic acid) (HY-78695), Black: linker (HY-W004640); Pink: E3 ligase ligand, L321 (HY-169359)) .
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- HY-140902A
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PROTAC Linkers
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Cancer
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Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs .
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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-161346
-
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ADC Cytotoxin
Epigenetic Reader Domain
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Cancer
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EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures .
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- HY-163826
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Ligands for E3 Ligase
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Cancer
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|
Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph is a ligand for E3 ubiquitin ligase. Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph can be connected to the ligand for protein by a linker to form 22-SLF (HY-163807) .
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-
- HY-143883
-
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PROTACs
Akt
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Cancer
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|
MS143 is a potent PROTAC AKT degrader (DC50=46 nM and GI50=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker) .
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- HY-157839
-
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PROTACs
α-synuclein
Tau Protein
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Neurological Disease
|
|
PROTAC α-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with EC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-synuclein degrader 6 plays an important role in neurodegenerative diseases (NDs) research (Blue:ubiquitin E3 ligase cereblon ligand (HY-14658), Black: linker (HY-128803); Pink: Ligand for target protein (HY-151035)) .
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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-110174
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α-synuclein
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Neurological Disease
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NAB2 is a neuron-protective agent. NAB2 strongly and selectively protects diverse cell types from α-syn toxicity. NAB2 promots endosomal transport events dependent on the E3 ubiquitin ligase Rsp5/Nedd4. NAB2 identifies a agentgable node in the biology of α-syn that can correct multiple aspects of its underlying pathology, including dysfunctional endosomal and endoplasmic reticulum-to-Golgi vesicle trafficking .
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- HY-159974
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Me-SJ46411-PEG1-Piperazine-Boc is a conjugate of E3 ubiquitin ligase and PROTAC linker, which can be used for the synthesis of PROTAC molecules. For example, Me-SJ46411-PEG1-Piperazine-Boc combined with target protein ligand (+)-JQ-1 (HY-13030) can be used to synthesize the selective BRD3 PROTAC degrader SJ46420 (HY-168635). .
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- HY-161960
-
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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EP300/CBP ligand 2 (compound S19) is a ligand targeting the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). EP300/CBP ligand 2 can be used as a target protein ligand in the PROTAC structure, and can be coupled to the E3 ubiquitin ligase ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, EP300/CBP ligand 2 can be coupled with the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc (HY-161961) to produce the PROTAC molecule dCE-2 (HY-161958) .
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- HY-129619
-
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SNIPERs
Estrogen Receptor/ERR
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Cancer
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|
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 .
|
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- HY-123941
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dTAG-7
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PROTACs
FKBP
Epigenetic Reader Domain
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Cancer
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|
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN .
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- HY-158036
-
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PROTACs
STING
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Others
Inflammation/Immunology
|
|
PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC50=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .
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- HY-130408
-
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ADC Linker
PROTAC Linkers
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Cancer
|
|
m-PEG6-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG6-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) .
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-
- HY-W018174
-
|
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ADC Linker
PROTAC Linkers
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Cancer
|
|
m-PEG3-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG3-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) .
|
-
- HY-126885
-
![4-Methylanisole-dihydrouracil-imidazo[1,2-a]pyridine-piperidine-NH-Boc](http://file.medchemexpress.com/product_pic/hy-163222.gif)
![Thalidomide-NH-C2-2-azaspiro[3.3]heptane](http://file.medchemexpress.com/product_pic/hy-168312.gif)
![(S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-C-Pip](http://file.medchemexpress.com/product_pic/hy-168310.gif)
