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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
173 Results for "
Target ability
" in MedChemExpress (MCE) Product Catalog:
Products (173)
173 Results for "Target ability" in MCE Product Catalog:
Cat. No.: HY-13976A
CAS No.: 51352-87-5
Target:
Research Areas:
PRL-8-53 is an orally active, blood-brain barrier-permeable benzoate derivative with potent spasmolytic activity and central nervous system regulatory activity. PRL-8-53 acts on dopamine, serotonin and cholinergic-related targets, enhances dopamine activity, partially inhibits serotonin function and elicits cholinergic responses, thereby maintaining neurotransmitter balance in the central nervous system. PRL-8-53 improves learning ability, short-term memory and long-term memory in animals. PRL-8-53 can be used in central nervous system-related research .
Cat. No.: HY-L907
12,373 compounds
The most prominent mechanism of action of kinase inhibitors is their competition with ATP by binding to the hinge region of the kinase protein. Once the kinase is blocked by an inhibitor, it loses the ability to transfer phosphate groups from ATP to other molecules, resulting in the loss of kinase activity.
The hinge-binding region of kinase inhibitors mimics the interaction pattern between the ATP nucleobase and the kinase. MCE extracted thousands of kinase inhibitors from the ChEMBL database and isolated their molecular fragments. In certain cases, the amino and amide groups on the molecular fragments are crucial for binding in the hinge region. Therefore, we enhanced the diversity of the collected results by adding these two groups to unoccupied positions on the ring system. Subsequently, the fragments were assessed for their hinge region binding ability via docking at distinct kinases, we also applied pharmacophore constraints to ensure interactions with key amino acids in the kinase hinge region, ultimately obtaining kinase-related molecular fragments.
MCE provides over 12,373 kinase fragment molecules that meet the above requirements and are available off the shelf, serving as an effective tool for screening and developing drugs targeting kinases.
Cat. No.: HY-182788
CAS No.: 3113741-59-3
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Multitarget AD-IN-7 is an orally active multi-target anti-AD compound. Multitarget AD-IN-7 exhibits inhibitory activity against GSK-3β and GSK-3α (IC50 = 0.66, 0.83 nM). Multitarget AD-IN-7 upregulates the expression of p-GSK-3β-Ser9, inhibits the phosphorylation of tau-Ser396, targets Aβ1-42, chelates pathogenic metal ions, scavenges ABTS•+, upregulates the expression of β-catenin and neurogenesis biomarkers, and promotes neurite outgrowth. Multitarget AD-IN-7 improves motor ability in Alzheimer's disease zebrafish. Multitarget AD-IN-7 is applicable to research related to Alzheimer's disease .
Cat. No.: HY-P10667
Cat. No.: HY-L027
1,237 compounds
Viruses are much simpler organisms than bacteria, and they are made from protein substances and nucleic acid. Despite the fact that the exact mechanism of infection is extremely specific to each type of virus, the general scheme of infection can be represented in the following manner: A virus is absorbed at the surface of a host cell and then permeates through the membrane, where it releases nucleic acid from its protein protection. Then the viral nucleic acid begins to replicate, and transcription of the viral genome takes place either in the cytoplasm, or in the nucleus of the host cell. As a result of these events, a large amount of viral nucleic acid and protein are made to make new generations of virions. Therefore, one mechanism of action of antiviral drugs is to interfere with the ability of a virus to get into a target cell. A second mechanism of action is to target the processes that synthesize virus components after a virus invades a cell, such as nucleotide or nucleoside analogs.
MCE designs a unique collection of 1,237 anti-virus compounds that target several viruses, including SARS-CoV, HBV, HCV, HIV, HSV and Influenza Virus. It’s an effective tool for anti-virus drug discovery.
Cat. No.: HY-183783
PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma .
Cat. No.: HY-18740
CAS No.: 79855-88-2
Synonyms: HL 725 free base
Target:
Research Areas:
Trequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia) .
Cat. No.: HY-18740A
CAS No.: 78416-81-6
Synonyms: HL 725
Target:
Research Areas:
Trequinsin hydrochloride (HL 725) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin hydrochloride targets PDE3 with an IC50 of <1 nM. Trequinsin hydrochloride enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin hydrochloride significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin hydrochloride exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin hydrochloride has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia) .
Cat. No.: HY-P11903
Research Areas:
Cat. No.: HY-116392E
CAS No.: 109836-82-0
Research Areas:
D-threo-PDMP is a potent glucoceramide synthase (GCS) inhibitor, which reduces the glycosphingolipids (such as GM3 and GD3) on the cell surface by inhibiting glycosylation, reduces the total length of the axon plexus and the number of axon branch points, and inhibits neurite growth. D-threo-PDMP inhibits the synthesis of GM3, thereby reducing the adhesion ability of B16 melanoma cells and mimicking the pathological effects of hyperglycemia/TGF-β1. D-threo-PDMP inhibits the synthesis of GD3, thereby protecting liver cells from apoptosis induced by TNF-α. D-threo-PDMP can be used to study diseases related to targeted glycosphingolipid metabolism .
Target:
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D-threo-PDMP hydrochloride is a potent glucoceramide synthase (GCS) inhibitor, which reduces the glycosphingolipids (such as GM3 and GD3) on the cell surface by inhibiting glycosylation, reduces the total length of the axon plexus and the number of axon branch points, and inhibits neurite growth. D-threo-PDMP hydrochloride inhibits the synthesis of GM3, thereby reducing the adhesion ability of B16 melanoma cells and mimicking the pathological effects of hyperglycemia/TGF-β1. D-threo-PDMP hydrochloride inhibits the synthesis of GD3, thereby protecting liver cells from apoptosis induced by TNF-α. D-threo-PDMP hydrochloride can be used to study diseases related to targeted glycosphingolipid metabolism .
Cat. No.: HY-178962
Target:
Research Areas:
Antitumor agent-207 (compound 10K) is a Pt(IV)-NO prodrug with high lipid solubility, good stability, and excellent tumor targeted release ability. Antitumor agent-207 has significant anti proliferative activity in various cells such as TE-1 (IC50 = 1.79 μM), TE-10 (IC50 = 1.95 μM), KYSE-30 IC50 = 5.99 μM), KYSE-520 (IC50 = 5.53 μM) cells. Antitumor agent-207 can significantly enhance intracellular Pt accumulation and DNA platformization levels, and effectively release NO. Antitumor agent-207 can be used for research on cancers such as esophageal cancer .
Cat. No.: HY-L0115V
10,091 compounds
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.
Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.
Cat. No.: HY-108036AR
CAS No.: 868156-46-1
Synonyms: (S)-Hydroxypropyl tetrahydropyrantriol (Standard)
Research Areas:
(S)-Pro-xylane (Standard) is the analytical standard of (S)-Pro-xylane (HY-108036A). This product is intended for research and analytical applications. (S)-Pro-xylane ((S)-Hydroxypropyl tetrahydropyrantriol) is a bioactive C-glycoside that targets the biosynthesis pathway of glycosaminoglycans/mucopolysaccharides (GAGs) in the sKin matrix and can be absorbed transdermally. (S)-Pro-xylane stimulates the biosynthesis of GAGs in fibroblasts, enhances the structural stability of the sKin extracellular matrix, improves sKin elasticity and moisturizing ability, and delays wrinkle formation. (S)-Pro-xylane can effectively promote the synthesis of collagen fibers and hyaluronic acid in the dermis. (S)-Pro-xylane is used in the field of anti-aging cosmetics to improve sKin hydration and elasticity. (S)-Pro-xylane is eco-friendly and biodegradable .
Cat. No.: HY-156045C
CAS No.: 9041-36-5
Cat. No.: HY-167832
CAS No.: 2059104-90-2
Target:
JNK SGK ROCK Tau Protein MMP DNA/RNA Synthesis Pyruvate Kinase NF-κB COX NO Synthase Reactive Oxygen Species (ROS)
Research Areas:
PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease .
Cat. No.: HY-W738256
CAS No.: 180152-82-3
Synonyms: MDTPA
Research Areas:
Maleimide-DTPA (MDTPA) is a maleimide-functionalized bifunctional chelator that enables site-specific conjugation via a thioether bond to single-domain antibody fragments (sdAb) containing free cysteine, and mediates 111In radiolabeling. DTPA-2Rs15d-HLC, formed by the conjugation of Maleimide-DTPA with anti-HER2 sdAb 2Rs15d-HLC, retains high affinity for HER2 with a Kd of 5.9 nM, and maintains targeting ability to HER2-positive cells and tumors after 111In labeling. Maleimide-DTPA can be used for radiotracer construction, SPECT molecular imaging, and HER2-positive tumor research .
Cat. No.: HY-153552
CAS No.: 2758337-19-6
NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis .
NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis .
Cat. No.: HY-162834
CAS No.: 2375564-54-6
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Research Areas:
PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research[1].
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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
