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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
20 Results for "
ligand efficiency
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "ligand efficiency" in MCE Product Catalog:
Cat. No.: HY-P5423
CAS No.: 107658-43-5
Cat. No.: HY-P10709
CAS No.: 847058-45-1
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DPyPE is a neutral phosphatidylethanolamine lipid composed of a polyisoprene alkyl chain with two pyridine-containing phosphine ligands. DPyPE is mainly used in liposome formulations and to enhance the efficiency of gene delivery in vitro and in vivo. For example, DPyPE can be mixed with cationic lipids such as VC1052 (HY-156616) (in a 1:1 ratio) to form the vaccine adjuvant Vaxfectin (HY-142998). DPyPE assists VC1052 in binding to negatively charged pDNA to form a uniform liposome complex by regulating the fluidity and stability of the liposome membrane .
Cat. No.: HY-P10489
CAS No.: 374675-19-1
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Cat. No.: HY-172699A
DSPE-PEG3400-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG3400-ANG can be used for drug delivery .
Cat. No.: HY-W023758
CAS No.: 166196-54-9
Synonyms: 4-(4-Bromo-1H-pyrazol-5-yl)pyridine
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HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
Cat. No.: HY-144456
CAS No.: 2276711-87-4
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Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model .
Cat. No.: HY-151387
CAS No.: 1784491-64-0
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A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases .
Cat. No.: HY-14863
CAS No.: 250384-82-8
Synonyms: CTA-018
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Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
Cat. No.: HY-172700
DSPE-PEG5000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG5000-ANG can be used for drug delivery .
Cat. No.: HY-135711
CAS No.: 1305116-69-1
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PDE8B-IN-1 is a selective inhibitor of phosphodiesterase 8B (PDE8B) with the activity of enhancing insulin secretion. PDE8B-IN-1 showed good efficacy in high-throughput screening and optimized its ligand efficiency through rapid deconstruction. PDE8B-IN-1 showed high target selectivity and good bioavailability in preclinical development, providing a basis for exploring its potential inhibitory use .
Cat. No.: HY-W003471
CAS No.: 159326-68-8
Pyrrolo[2,1-f][1,2,4]triazin-4-amine is a MAP4K4 inhibitor with a surface plasmon resonance (SPR) Kd of 88 μM and a ligand efficiency of 0.56 .
Cat. No.: HY-172698
DSPE-PEG1000-ANG is a PEG compound which composed of DSPE and a dual-targeting ligand (Angiopep-2, ANG). ANG exhibits high LRP1 binding efficiency and has been used for glioma-targeting delivery. DSPE-PEG1000-ANG can be used for drug delivery .
Cat. No.: HY-W075745
CAS No.: 2049086-35-1
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SK-J003-1n is a nickel catalyst with excellent cross-coupling reaction activity. SK-J003-1n can be used as a ligand in organic synthesis to improve the selectivity and efficiency of the reaction. SK-J003-1n can effectively catalyze the coupling reaction between different substrates, highlighting its important role in compound development and material science.
Cat. No.: HY-L151
555 compounds
PROTACs (Proteolysis-targeting chimeras) is a class of molecules that utilize ubiquitin-proteasome system (UPS) to ubiquitinate and degrade target proteins. The PROTACs molecule consists of two ligands joined by a linker. The one-to-one interaction between PROTACs and target proteins determines the high efficiency of PROTACs, making it a potential molecule for targeted protein degradation (TPD) therapy.
MCE supplies a unique collection of 555 PROTACs that effectively degrade target proteins with more powerful screening capability. MCE PROTAC Library is a useful tool for signal pathway research, protein degradation therapy research, drug discovery and drug repurposing, etc.
Cat. No.: HY-P11903
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dTBP-3 is a fully D-configured polypeptide competitive inhibitor that targets TIGIT. dTBP-3 can competitively occupy the binding interface between TIGIT and its ligand PVR, block TIGIT-mediated immunosuppressive signals, and reverse the immune exhaustion of NK cells and CD8 + T cells . dTBP-3 possesses anti-proteolytic activity and tumor tissue penetration ability, and can also enhance the tumor penetration capacity and cellular internalization efficiency of nanocarriers. dTBP-3 can be used in studies related to liver cancer, triple-negative breast cancer and non-small cell lung cancer .
Cat. No.: HY-189243
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P2Y2R antagonist-2 is an antagonist of the P2Y2 receptor (P2Y2R), with a pKi value of 6.53 for human P2Y2R. P2Y2R antagonist-2 blocks UTPγS (HY-137603)-induced calcium mobilization, binds to the orthosteric site of P2Y2R to displace fluorescent antagonist ligands, and forms unique binding interactions. P2Y2R antagonist-2 has no structural alerts, exhibiting low lipophilicity and high lipophilic efficiency. P2Y2R antagonist-2 can be used in studies related to astrocytoma and inflammation .
Cat. No.: HY-L256
100 compounds
In modern drug discovery and chemical biology research, the azide group (-N3) is an important functional moiety that is widely used in click chemistry, biomolecular labeling, drug delivery systems, and prodrug design due to its unique reactivity and bioorthogonality.
The MCE Azide Structural Compound Library contains 100 compounds featuring -N3 functional groups. It is designed for the construction of click chemistry reaction systems and the subsequent development of functional molecules. This library enables the rapid assembly of targeting ligands, linkers, and functional molecular modules, thereby accelerating PROTAC assembly, optimization of antibody-drug conjugate (ADC) linkers, and the development of biological labeling probes. In addition, the high reaction selectivity and excellent biocompatibility of the azide group allow it to maintain stable reactivity even in complex biological environments, improving controllability and efficiency in drug design. It serves as an indispensable molecular tool in modern medicinal chemistry and chemical biology research.
Cat. No.: HY-L109
836 compounds
Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs.
However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.
With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 836 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.
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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
