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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
21 Results for "
small-molecule PROTACs
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "small-molecule PROTACs" in MCE Product Catalog:
8
8 Cited Publications
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MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Synonyms: 2-Azidoacetic acid
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Azidoacetic Acid (2-Azidoacetic acid) (compound 92-1) is a click chemistry reagent containing an azide group. Azidoacetic Acid can be used as a small molecule tool for the synthesis of PROTAC . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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C004019 is a BBB-penetrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases .
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Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31 comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
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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 .
Cat. No.: HY-131203
CAS No.: 2410947-56-5
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .
Cat. No.: HY-157558
CAS No.: 3093556-86-3
Synonyms: 8SGE
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KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-W877989
CAS No.: 2241315-66-0
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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 .
Cat. No.: HY-157559
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KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-400766
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BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
Cat. No.: HY-12863B
CAS No.: 1380089-81-5
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CPI-0610 carboxylic acid is a novel small-molecule bromodomain and extraterminal protein inhibitor for the treatment of multiple myeloma. CPI-0610 carboxylic acid binds to the N-terminal bromodomains of BRD2, BRD3, BRD4, and BRDT, as well as the BRD9 bromodomain. CPI-0610 carboxylic acid can serve as a target protein ligand for the synthesis of PROTAC. CPI-0610 carboxylic acid can be used for research on multiple myeloma, acute myeloid leukemia, and lung and cervical cancers .
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(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) .
Cat. No.: HY-401056
CAS No.: 3032602-27-7
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BWA-522 intermediate-3 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
Cat. No.: HY-L128
184 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.
Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).
MCE carefully prepared a unique collection of 184 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.
Cat. No.: HY-L934
122 compounds
CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein.
These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins.
MCE compiles 122 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.
Cat. No.: HY-184991
CAS No.: 2982853-56-3
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AK305 is a small-molecule ligand for the SH2 domains of STAT5A, STAT5B and STAT6, with a Ki of 0.4 μM for STAT6 and a Ki of 1.0 μM for both STAT5A and STAT5B. AK305 exhibits only very low or no cell growth inhibitory activity in leukemia cells and does not alter STAT protein levels. AK305 serves as the STAT5 ligand for AK-2292 (HY-148813), a STAT5 PROTAC degrader. AK305 can be used in the research of acute myeloid leukemia .
Cat. No.: HY-L129
130 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.
MCE carefully prepared a unique collection of 130 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.
Cat. No.: HY-181759
CAS No.: 3086024-48-5
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CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers .
Cat. No.: HY-L951
505 compounds
Macrocyclic scaffolds are increasingly valued in modern drug discovery for their exceptional activity against undruggable targets (proteases, kinases, PPIs). 2026 marks a key commercial breakthrough for oral macrocyclic peptides: enlicitide, the world’s first oral PCSK9 macrocyclic peptide, has received FDA approval. Macrocyclic candidates targeting KRAS and other classic undruggable targets have also entered clinical development, validating macrocyclization as an effective strategy to overcome druggability barriers.
Two core R&D directions lead current macrocyclic drug design: AI-driven de novo generation and structural optimization of small-molecule macrocycles, and macrocyclic peptides based on sequence design and conformational engineering. Macrocycle druggability hinges on embedded linkers, which determine cyclization efficiency, final conformation and drug-like properties. Bifunctional reaction orthogonality is the core linker selection criterion. Our linker library enables stepwise intramolecular cyclization with suppressed side reactions, accommodates varied ring sizes, and covers three key reaction systems: amide condensation, nucleophilic substitution and CuAAC click chemistry.
Built on classical macrocyclization systems, the library is processed through reaction classification, bifunctional orthogonality evaluation, novelty clustering and redundancy removal, with PROTAC long-chain and ADC cleavable linkers explicitly excluded. Featuring rigid, semi-rigid and flexible scaffolds, it is widely applicable to small-molecule macrocycle synthesis and linear peptide cyclization.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
