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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-W109760
CAS No.: 560088-89-3
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FmocNH-PEG2-CH2CONH-PEG2-CH2COOH is an optimized, extended PEG-like linker [1] .
Cat. No.: HY-19072
CAS No.: 84768-09-2
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BRL-36378 is an ACE inhibitor that inhibits angiotensin-converting enzyme activity. BRL-36378 can be used in ligand-based virtual screening to identify new leading structures for chemical optimization .
Cat. No.: HY-12625A
CAS No.: 1560968-55-9
MIV-6R is an optimized small molecule inhibitor of menin-mixed lineage leukemia (MLL) interaction with IC50 = 56 nM, and its specific mechanism of action activity has been validated in MLL leukemia cells.
Cat. No.: HY-15980
CAS No.: 1310455-86-7
GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
Cat. No.: HY-10030
CAS No.: 1037309-45-7
Synonyms: PF-2545920 succinate
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Mardepodect succinate (PF-2545920 succinate) is a potent and specific phosphodiesterase 10A (PDE10A) inhibitor with potential activity in the treatment of schizophrenia. Mardepodect succinate has been further optimized to improve brain penetration and compound-like properties for use in schizophrenia research .
Cat. No.: HY-160064
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SW1-A aptamer sodium is an optimized aptamer based on SW1 aptamer (HY-160063) that specifically targets liver cancer SMMC-7721 cells (Kd: 133.73 nM). SW1-A aptamer maintains strong affinity to liver cancer tissues and cells .
Cat. No.: HY-119185
CAS No.: 893556-15-5
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AZD-6605 is a potent, reversible inhibitor of MMP2, MMP9, MMP12 and MMP13 with excellent selectivity. During drug development, AZD-6605 was optimized for activity, solubility and DMPK properties against MMP13 by replacing the zinc hydroxide binding group associated with historical inhibitors .
Cat. No.: HY-143499
CAS No.: 2581113-51-9
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hMAO-B-IN-3 (Compound 15) is a potent inhibitor of hMAO-B with an IC50 of 47.4 nM. hMAO-B-IN-3 is playing favourable agent-like properties and a broad safety window. hMAO-B-IN-3 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands .
Cat. No.: HY-163518
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Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity .
Cat. No.: HY-14297
CAS No.: 652990-07-3
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Milveterol is a long-acting β(2)-adrenoceptor agonist with high binding activity. Milveterol exhibits high potency in vitro and a prolonged duration of action in a guinea pig bronchoprotection model. Milveterol has been structurally optimized to show enhanced binding potency compared to its parent monomer .
Cat. No.: HY-117697
CAS No.: 1290133-16-2
Lu AF11205 is a mGlu5 receptor positive allosteric modulator with activity modulating mGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.
Cat. No.: HY-W012935
CAS No.: 50675-20-2
Synonyms: Piperidine-4-carboxaldehyde
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Piperidine-4-carbaldehyde (Piperidine-4-carboxaldehyde) is a PROTAC Linker. Piperidine-4-carbaldehyde can be used to optimize combined with the target protein affinity, thus improve the PROTAC the molecular degradation efficiency. Piperidine-4-carbaldehyde can be used in the CDK2 PROTACs (HY-161708) .
Cat. No.: HY-146203
CAS No.: 2410056-27-6
Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
Cat. No.: HY-157444
CAS No.: 1613308-63-6
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5,3',4',3'',4'',5''-6-O-Ethyl-EGCG (Y6) is a potent adjuvant obtained by optimization of the structure of EGCG. 5,3',4',3'',4'',5''-6-O-Ethyl-EGCG (Y6) decreases the expression of HIF-1α and CBR1 at both the mRNA and protein levels .
Cat. No.: HY-176512
CAS No.: 3100308-37-7
FO-32 is an ionizable lipid and mRNA delivery carrier with state-of-the-art aerosolized mRNA delivery capability. FO-32 delivers mRNA to mouse muscle, nasal mucosa, lung, as well as ferret lung epithelium (including conducting airways). FO-32 can be used in studies related to the generation of lipid nanoparticles (LNPs) and the optimization of drug delivery .
Cat. No.: HY-109743
CAS No.: 1000036-77-0
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BP14979 is a dopamine D3 receptor agonist with activity in the study of neurological diseases. BP14979 can be used to develop ligands with higher selectivity and affinity for D3 receptors. The structural characteristics of BP14979 make it potential in modulating the efficacy of D3 receptors. The design of BP14979 is based on the difference in efficacy with D3R selective antagonists, providing opportunities for optimizing new drug development .
Cat. No.: HY-175639
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ALR2-IN-8 is a potent aldose reductase (ALR2/AKR1B1) inhibitor with a KI of 7.34 nM. ALR2-IN-8 has extremely low toxicity to normal cells and has a weak direct killing effect on cancer cells. ALR2-IN-8 can used for the studies of diabetic and inflammation-linked disorders .
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.
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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
