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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
9327 Results for "
linking
" in MedChemExpress (MCE) Product Catalog:
Products (9327)
9327 Results for "linking" in MCE Product Catalog:
Cat. No.: HY-151833
CAS No.: 2639395-39-2
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Methyltetrazine-amido-N-bis(PEG4-acid) is a click chemistry reagent containing an azide group. Methyltetrazine-amido-N-bis(PEG4-acid) is a PEG derivative that contains a methyltetrazine group and two acid groups. This reagent can react with TCO-containing compounds to form a stable covalent bond without the catalysis of Cu or elevated temperatures. The inverse-electron demand Diels-Alder cycloaddition reaction of TCO with tetrazines is the fastest bioorthogonal reaction with exceptional selectivity. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. PEG linker increases the water solubility of the compound. Reagent grade, for research use only . Methyltetrazine-amido-N-bis(PEG4-acid) is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
Cat. No.: HY-162098
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PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
Cat. No.: HY-180989
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PROTAC PLK1 Degrader-2 is a peptide-based N-end rule PLK1 mini-PROTAC. PROTAC PLK1 Degrader-2 utilizes Arg12 as dual-function cell-permeable N-degron to recruit UBR1/UBR2 E3 ligases, mediates PLK1 ubiquitination and proteasome-dependent degradation. PROTAC PLK1 Degrader-2 suppresses cervical cancer cell proliferation, induces G2/M cell cycle arrest and tumor cell apoptosis, and exerts potent in vivo anti-tumor efficacy in mice and can be applied to research on PLK1-driven cervical carcinoma (PLK1 ligand: POI ligand-3 (HY-180990); E3 ligase ligand: Arg12 (HY-P11631); PROTAC linker: 6-Aminocaproic acid (HY-B0236)) .
Cat. No.: HY-181907
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NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C) .
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
Cat. No.: HY-187534
VEGFR2 AUTOTAC-1 is a VEGFR2 AUTOTAC degrader. VEGFR2 AUTOTAC-1 recruits p62, activates the autophagy-lysosome pathway through the p62-LC3 axis cascade, forms a ternary complex with VEGFR2 and p62, and drives UPS-independent post-translational degradation of VEGFR2. VEGFR2 AUTOTAC-1 induces G1 phase arrest and endogenous apoptosis in cells via the mitochondrial and caspase apoptotic pathways, thereby inhibiting cancer cell proliferation, migration and malignant phenotypes; meanwhile, it inhibits endothelial cell tube formation, migration and endothelial-mesenchymal transition by regulating E-cadherin and MMP2. VEGFR2 AUTOTAC-1 is applicable to research related to triple-negative breast cancer.(Pink: VEGFR2 target protein ligand (HY-187558); Blue: p62 ligand (HY-W014292); Black: Linker)
Cat. No.: HY-E70065
CAS No.: 71124-51-1
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alpha-2,3-Sialyltransferase (PmST2) is a monofunctional α2-3 sialyltransferase that belongs to the GT52 family of Carbohydrate-Active enZymes (CAZy). alpha-2,3-Sialyltransferase (PmST2) catalyzes the transfer of sialic acid from CMP-Neu5Ac to the C3 position of galactose in lactosyl lipids, β1-4 linked galactosyl disaccharide lipids, and β-galactosyl monosaccharide lipids, with its catalytic activity decreasing sequentially toward these substrate classes. The function ofalpha-2,3-Sialyltransferase (PmST2) is independent of divalent metal cations and disulfide bonds, and it retains α2-3 sialyltransferase activity over a pH range of 4.5-10.0, with optimal activity observed at pH 6.0 .
Cat. No.: HY-P991402
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Cat. No.: HY-P992061
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Cat. No.: HY-W006886
CAS No.: 945212-26-0
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Cat. No.: HY-Y0850U1
CAS No.: 9002-89-5
Synonyms: Polyvinyl alcohol (Mw 61000, 98-99% hydrolyzed, ~1400 polymerization); Poly(Ethenol) (Mw 61000, 98-99% hydrolyzed, ~1400 polymerization)
Cat. No.: HY-L129
128 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 128 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-L054
379 compounds
Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.
MCE Endoplasmic Reticulum Stress Compound Library contains 379 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.
Cat. No.: HY-L020
654 compounds
The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells. The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development.
MCE designs a unique collection of 654 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.
Cat. No.: HY-163099
CAS No.: 2928571-43-9
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P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
Cat. No.: HY-164429
CAS No.: 2418533-90-9
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
Cat. No.: HY-164702
Synonyms: Izalontamab Brengitecan
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BL-B01D1 (Izalontamab Brengitecan) is a bispecific antibody-drug conjugate (ADC) targeting EGFR and HER3, formed by conjugating the EGFR/HER3 bispecific antibody Izalontamab (HY-P99676) to a novel TOP-I inhibitor payload Deruxtecan 2-hydroxypropanamide (HY-153891) via a cleavable linker (Mc-Gly-Gly-Phe-Gly). BL-B01D1 binds to EGFR and HER3 on the surface of tumor cells, mediates endocytosis and releases the payload, inhibits topoisomerase I, blocks DNA replication and RNA synthesis, and disrupts DNA structure. BL-B01D1 induces cell cycle S-phase arrest, apoptosis, antibody-dependent cell-mediated cytotoxicity, and tumor cell death. BL-B01D1 can be used for cancer research .
Cat. No.: HY-176220
CAS No.: 3060458-90-1
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GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
Cat. No.: HY-184158
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HATC is a HIF-1α AUTAC degrader. HATC links HIF-1α to LC3 to form a ternary complex that undergoes degradation via the autophagy-lysosome fusion pathway. HATC induces dose-dependent HIF-1α degradation in multiple cell types. HATC reduces visceral fat accumulation, hepatic lipid deposition, senescent cell aggregation, and bone loss; alleviates age-related intervertebral disc degeneration, liver dysfunction, kyphosis, and alveolar dilation; decreases circulating lactic acid levels; improves physical performance; and reverses age-related changes in granulocyte proportions. HATC extends median and maximum lifespan, reduces transcriptomic age, and causes no obvious persistent toxicity. HATC can be used in the research of age-related diseases (pink: LC3 ligand (HY-50759); blue: HIF-1α ligand (HY-P10426); Linker: (HY-W008264)) .
Cat. No.: HY-185743
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ZW-191 is an antibody-drug conjugate (ADC) targeting folate receptor α (FRα). ZW-191 consists of ZW-191 Antibody (HY-P992515) as the antibody component and MC-GGFG-AM-(10Me-11F-Camptothecin) (HY-153360) as the linker-payload component. ZW-191 possesses excellent tumor sphere penetration, cellular internalization and payload delivery capabilities, and can release a topoisomerase 1 inhibitor inside tumor cells to inhibit tumor cell activity. ZW-191 exerts a potent bystander effect on both antigen-positive and antigen-negative cells. ZW-191 exhibits prominent activity in xenograft models of cell lines with different FRα expression levels. ZW-191 can be used in studies related to ovarian cancer, non-small cell lung cancer, endometrial cancer and triple-negative breast cancer .
Cat. No.: HY-N16300
CAS No.: 3091879-75-0
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Mito-laurdan (bromide) is a Fluorescent dye for mitochondrial membrane fluidity and packing measurement. It depends on membrane potential for targeting: it contains a cationic triphenylphosphonium moiety that accumulates at the inner mitochondrial membrane due to the membrane's negative potential, connected via a 3-carbon linker. As a solvatochromic dye derived from Laurdan (HY-D0080), it retains the characteristic mechanism where fluorescence emission shifts based on membrane packing: in more fluid, loosely packed membranes, greater water penetration leads to increased dipolar relaxation and a bathochromic red shift in emission, while more ordered membranes show a blue-shifted emission; these shifts are quantified using generalized polarization, calculated from emission intensities in ordered and disordered spectral windows. Its excitation wavelength is 352 nm, with emission detected in ordered (409-463 nm) and disordered (473-516 nm) spectral windows. It localizes specifically to mitochondria in HeLa cells, showing high signal overlap with MitoTracker Deep Red, and can detect changes in inner mitochondrial membrane fluidity .
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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
