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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
205 Results for "
OPTimization
" in MedChemExpress (MCE) Product Catalog:
Products (205)
205 Results for "OPTimization" in MCE Product Catalog:
Cat. No.: HY-179626
CAS No.: 2138299-66-6
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STING agonist-49 (Compound 1) is a STING agonist and can be used as a payload for ADCs. STING agonist-49 can be applied in lung cancer research .
Cat. No.: HY-180452
CAS No.: 2998560-77-1
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HAT-IN-10 (Compound 12a) is an anti-human African trypanosomiasis (HAT) agent, with an EC50 value of 0.23 μM for T. brucei. HAT-IN-10 can be used for research on HAT .
Cat. No.: HY-129836R
CAS No.: 26889-93-0
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L-Amoxicillin (Standard) is the analytical standard of L-Amoxicillin. This product is intended for research and analytical applications. L-Amoxicillin is an antibiotic with activity against a wide range of bacterial infections. L-Amoxicillin is commonly used in antibacterial combinations when used in combination with the β-lactamase inhibitor potassium clavulanic acid. The related substances analysis method for L-Amoxicillin has been developed and validated according to the International Conference on Harmonization (ICH) guidelines, ensuring its effectiveness and accuracy in mixtures. L-Amoxicillin and some of its impurities have been further analyzed in stress testing and stability studies, providing support for optimizing its application .
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Exo-1,4-β-xylosidase is an exonuclease that specifically acts on the β-1,4 glycosidic bonds at the non-reducing ends of xylan and xylooligosaccharides. Exo-1,4-β-xylosidase is Ca 2+-dependent and reversibly binds to metal ions to catalyze the hydrolysis of β-1,4 glycosidic bonds, thereby degrading xylan to produce xylose. Exo-1,4-β-xylosidase can be used in research fields such as lignocellulose bioconversion, bioethanol production, and optimization of xylan saccharification processes .
Cat. No.: HY-W743258
Cat. No.: HY-159771
CAS No.: 3095069-75-0
Cat. No.: HY-P11398
Cat. No.: HY-117380
CAS No.: 224961-34-6
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SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .
Cat. No.: HY-177554
CAS No.: 2724919-69-9
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KB05yne is a site-selective, alkyne-functionalized electrophilic "probe" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1) but does not label their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for the discovery and optimization of site-specific covalent ligands, and is applicable to proteins with diverse structures and functions, especially in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins .
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Cat. No.: HY-K0606
MCE Methenamine Silver Stain Kit For Basement Membrane (PASM) is developed based on the classical staining principle. Through an optimized staining system and standardized reagent combination, it enables clear visualization of basement membranes and related reticular structures in tissue sections. This method is particularly widely used in renal pathology research, where it is commonly applied to examine morphological alterations of the glomerular capillary basement membrane, such as thickening, rupture, folding, double-contour (tram-track) appearance, or abnormal proliferation caused by inflammatory injury. In addition, this method can also be applied to the histological investigation and morphological observation of glomerular diseases, diabetic nephropathy, and other basement membrane–associated pathological changes.
Cat. No.: HY-L935
1039 compounds
POI (Protein of Interest) refers to the target protein, namely the disease-causing protein or key functional protein that undergoes degradation or functional modulation in molecular glue-mediated processes. The Molecular Glue POI Library consists of a series of fragments that can specifically bind to different types of POIs. As key components of molecular glues, these ligands form stable interactions with target proteins, laying the foundation for molecular glues to induce the interaction between POIs and E3 ubiquitin ligases. The covered POIs include various types such as cancer-associated GSPT1, androgen receptors, and abnormally aggregated proteins linked to neurodegenerative diseases.
This fragment library can be applied to the screening and optimization of targeted protein degraders. By screening ligands with high affinity and strong selectivity for specific POIs from the library, core structures can be identified to develop novel molecular glues. For instance, optimization of ligands targeting GSPT1 has yielded molecular glue degraders with enhanced degradation activity. Since many POIs are difficult to drug due to the lack of traditional small-molecule binding pockets, some ligands in the POI Ligand Library can modulate such POIs by inducing protein-protein interactions, thereby further expanding the scope of drug discovery for undruggable targets.
MCE has compiled a POI Fragment Library comprising thousands of POI fragments with molecular weights ranging from 150 to 400. This compound library can be widely applied in Molecular Glue research and development.
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exo-β-1,4-xylosidase,Clostridium stercorarium (EC.3.2.1.37) is an exonuclease that specifically acts on the β-1,4 glycosidic bonds at the non-reducing ends of xylan and xylooligosaccharides. exo-β-1,4-xylosidase is Ca 2+-dependent and reversibly binds to metal ions to catalyze the hydrolysis of β-1,4 glycosidic bonds, thereby degrading xylan to produce xylose. exo-β-1,4-xylosidase can be used in research fields such as lignocellulose bioconversion, bioethanol production, and optimization of xylan saccharification processes .
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exo-β-1,4-xylosidase, Bacteroides ovatus (EC.3.2.1.37) is an exonuclease that specifically acts on the β-1,4 glycosidic bonds at the non-reducing ends of xylan and xylooligosaccharides. exo-β-1,4-xylosidase is Ca 2+-dependent and reversibly binds to metal ions to catalyze the hydrolysis of β-1,4 glycosidic bonds, thereby degrading xylan to produce xylose. exo-β-1,4-xylosidase can be used in research fields such as lignocellulose bioconversion, bioethanol production, and optimization of xylan saccharification processes .
Cat. No.: HY-133031A
CAS No.: 474084-56-5
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CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
Cat. No.: HY-145432
CAS No.: 2747100-02-1
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents .
NMT-IN-1 is a Trypanosoma brucei N-myristoyltransferase (TbNMT) inhibitor, with an IC50 of 31 μM against TbNMT and an IC50 of 66 μM against hNMT. As a thiazolidinone hit compound identified via virtual screening, NMT-IN-1 exerts enzymatic inhibitory effects by binding to the active site of TbNMT. NMT-IN-1 adopts a binding mode distinct from that of pyrazole sulfonamide inhibitors and can inhibit the myristoyl transfer reaction catalyzed by TbNMT. NMT-IN-1 is mainly used in the research of anti-parasitic lead compounds for human African trypanosomiasis (African sleeping sickness). It provides a structural basis for the subsequent optimization of TbNMT inhibitors with high activity, high selectivity and blood-brain barrier permeability .
Cat. No.: HY-W237439
CAS No.: 958712-85-1
SEN205A is a fragment compound that binds to the hydrophobic pocket of human S100B (Kd=0.5-1.0 mM), which is the key region for the interaction of S100B with TRTK-12 and p53, and SEN205A can be displaced from this site by TRTK-12. SEN205A exhibits excellent in vitro ADME properties, including high metabolic stability, chemical stability, and good solubility under physiological pH conditions. SEN205A can serve as a starting fragment for structure-based optimization to develop inhibitors targeting the S100B-p53 protein-protein interaction and investigate the pathogenesis of malignant melanoma .
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.
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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
