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Results for "

Ligand efficiency

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Acetyl-CoA Carboxylase (1) Adenosine Receptor (1) Collagen (1) Cytochrome P450 (1) DNA/RNA Synthesis (1) Ephrin Receptor (1) Exosomes (1) IKK (1) Interleukin Related (1) JAK (1) Kisspeptin Receptor (1) Liposome (5) MAP4K (1) Phosphodiesterase (PDE) (1) PROTACs (2) Protease Activated Receptor (PAR) (1) ROR (1) SDCBP (1) SGK (1) VD/VDR (1) Xanthine Oxidase (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (2) Endocrinology (1) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (1)
Oligonucleotides:	Pegylated Lipids (3) Phospholipids (1)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Oligonucleotides

Targets Recommended: Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P5423

GALA	Exosomes Liposome	Cancer
GALA is a pH-responsive amphipathic peptide consisting of 30 amino acids, which acts as a lung endothelium-targeting ligand. GALA undergoes a conformational transition from random coil to α-helix in an acidic environment at pH 5.0, thereby inducing endosomal membrane destabilization and fusion. GALA-modified liposomes traverse lung endothelial cells via clathrin-dependent endocytosis and transcytosis, and specifically accumulate in the lungs after intravenous injection. GALA significantly promotes the cytosolic release of cargos carried by exosomes, plasmids and liposomes, effectively enhances gene transfection efficiency, and drives gene knockdown of functional macromolecules (such as siRNA) in alveolar epithelial cells (with no significant cytotoxicity at effective concentrations). GALA serves as a critical tool for studies on lung cancer metastasis (e.g., melanoma lung metastasis) and lung-targeted drug delivery systems .

HY-P10709

CREKA peptide	Collagen	Cardiovascular Disease Cancer
CREKA peptide is a selective non-covalent binding agent targeting fibrin, type IV collagen, and fibronectin, often used as a targeting ligand to modify delivery carriers. CREKA peptide specifically recognizes fibrin, fibronectin, and type IV collagen that are excessively deposited in the tumor microenvironment or fibrotic tissue, mediating the targeted accumulation of the carrier at the lesion site and promoting drug internalization into target cells (such as cancer cells and activated hepatic stellate cells). CREKA peptide can enhance targeted delivery efficiency, increase drug concentration at the lesion site, and reduce systemic side effects .

HY-112557

PROTAC TBK1 degrader-2 1 Publications Verification	PROTACs IKK	Cancer
PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC₅₀=15 nM; K_d=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC₅₀=8.7 nM), with low selectivity over TBK1 (IC₅₀=1.3 nM) .

HY-112766

DPyPE	Liposome	Others
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 .

HY-P10489

Kisspeptin-14 human	Kisspeptin Receptor	Cancer
Kisspeptin-14 human is a peptide hormone encoded by the KiSS-1 gene. Kisspeptin-14 human, along with several other similar peptide hormones, is produced from a common precursor protein by cleavage by different proteases. Kisspeptin-14 human is an endogenous ligand of KISS1R. Kisspeptin-14 human has the same receptor binding efficiency and potency as full-length kisspeptin. Kisspeptin-14 human binds to its receptor GPR54 and is able to activate this G protein-coupled receptor and activate multiple intracellular signaling pathways. Kisspeptin-14 human can be used to study reproductive development and tumor metastasis .

HY-172699A

DSPE-PEG3400-ANG	Liposome	Cancer
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 .

HY-147376

hACC2-IN-1	Acetyl-CoA Carboxylase	Metabolic Disease
hACC2-IN-1 is a potent acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC₅₀ value of 2.5 μM (hACC2). hACC2-IN-1 could be used for obesity research .

HY-149204

SYNTi	SDCBP	Cancer
SYNTi is a PDZ domain inhibitor targeting the syndecan/syntenin protein-protein Interaction. SYNTi exhibits an IC₅₀ value of 400 nM and ligand efficiency (LE) value of 0.24. SYNTi can be used for breast cancer research .

HY-176823

PROTAC SGK3 degrader-2	PROTACs SGK	Cancer
PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC₅₀ values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation. (Pink: SGK3 ligand (HY-167701), Blue: VHL Ligand (HY-120217A), Black: Linker (HY-130618), SGK3 ligand-linker conjugate (HY-176824)) .

HY-W023758

HDGFRP2/PSIP1-IN-1 4-(4-Bromo-1H-pyrazol-5-yl)pyridine	DNA/RNA Synthesis	Cancer
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 K_d value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a K_d value of 27 μM; meanwhile, it has a K_d value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .

HY-178282

JAK1-IN-19	JAK	Inflammation/Immunology
JAK1-IN-19 (Compound 18) is a potent JAK1 inhibitor with IC₅₀s of 0.02, 0.5, 91 and 0.2 nM against JAK1, JAK2, JAK3 and TYK2. JAK1-IN-19 exhibits improved rat and human intrinsic clearance. JAK1-IN-19 can be used for the studies of atopic dermatitis and other autoimmune diseases .

HY-144456

Xanthine oxidase-IN-5	Xanthine Oxidase	Metabolic Disease
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 .

HY-151387

A2AAR antagonist 1	Adenosine Receptor	Neurological Disease
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a K_i value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases .

HY-143315

Protease-Activated Receptor-1 antagonist 3	Protease Activated Receptor (PAR)	Cardiovascular Disease
Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC₅₀ value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K ⁺ channel with an IC₅₀ value of 9 µM .

HY-14863

Lunacalcipol CTA-018	VD/VDR Cytochrome P450	Others Endocrinology
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) .

HY-172700

DSPE-PEG5000-ANG	Liposome	Cancer
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 .

HY-135711

PDE8B-IN-1	Phosphodiesterase (PDE)	Metabolic Disease
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 .

HY-W003471

Pyrrolo[2,1-f][1,2,4]triazin-4-amine	MAP4K	Others
Pyrrolo[2,1-f][1,2,4]triazin-4-amine is a MAP4K4 inhibitor with a surface plasmon resonance (SPR) K_d of 88 μM and a ligand efficiency of 0.56 .

HY-10654

EphB4-IN-2	Ephrin Receptor	Cancer
EphB4-IN-2 (compound 66) is a tyrosine kinase inhibitor with an IC₅₀ value of 1.6 nM against human EphB4, and exhibits selectivity toward kinases bearing threonine gatekeeper residues. EphB4-IN-2 also has high ligand efficiency .

HY-172698

DSPE-PEG1000-ANG	Liposome	Cancer
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 .

HY-180813

RORγ-IN-3	ROR Interleukin Related	Inflammation/Immunology
RORγ-IN-3 (Compound 21) is a potent and highly selective RORγ inhibitor with an EC₅₀ of 84 nM. RORγ-IN-3 can effectively inhibit the production of IL-17, with an IC₅₀ value of 1.0 μM. RORγ-IN-3 can be used for the study of autoimmune diseases .

HY-W075745

SK-J003-1n	Others
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.	Product Name

HY-L151

PROTAC Library	515 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 515 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.

PROTAC Library

515 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 515 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.

HY-L109

Protein-protein Interaction Inhibitor Library	782 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 782 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.

Protein-protein Interaction Inhibitor Library

782 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 782 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.

Cat. No.	Product Name	Type

HY-172699A

DSPE-PEG3400-ANG	Biochemical Assay Reagents
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 .

HY-172700

DSPE-PEG5000-ANG	Biochemical Assay Reagents
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 .

HY-172698

DSPE-PEG1000-ANG	Biochemical Assay Reagents
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.	Product Name	Target	Research Area

HY-P5423

GALA	Exosomes Liposome	Cancer
GALA is a pH-responsive amphipathic peptide consisting of 30 amino acids, which acts as a lung endothelium-targeting ligand. GALA undergoes a conformational transition from random coil to α-helix in an acidic environment at pH 5.0, thereby inducing endosomal membrane destabilization and fusion. GALA-modified liposomes traverse lung endothelial cells via clathrin-dependent endocytosis and transcytosis, and specifically accumulate in the lungs after intravenous injection. GALA significantly promotes the cytosolic release of cargos carried by exosomes, plasmids and liposomes, effectively enhances gene transfection efficiency, and drives gene knockdown of functional macromolecules (such as siRNA) in alveolar epithelial cells (with no significant cytotoxicity at effective concentrations). GALA serves as a critical tool for studies on lung cancer metastasis (e.g., melanoma lung metastasis) and lung-targeted drug delivery systems .

HY-P10709

CREKA peptide	Collagen	Cardiovascular Disease Cancer
CREKA peptide is a selective non-covalent binding agent targeting fibrin, type IV collagen, and fibronectin, often used as a targeting ligand to modify delivery carriers. CREKA peptide specifically recognizes fibrin, fibronectin, and type IV collagen that are excessively deposited in the tumor microenvironment or fibrotic tissue, mediating the targeted accumulation of the carrier at the lesion site and promoting drug internalization into target cells (such as cancer cells and activated hepatic stellate cells). CREKA peptide can enhance targeted delivery efficiency, increase drug concentration at the lesion site, and reduce systemic side effects .

HY-P10489

Kisspeptin-14 human	Kisspeptin Receptor	Cancer
Kisspeptin-14 human is a peptide hormone encoded by the KiSS-1 gene. Kisspeptin-14 human, along with several other similar peptide hormones, is produced from a common precursor protein by cleavage by different proteases. Kisspeptin-14 human is an endogenous ligand of KISS1R. Kisspeptin-14 human has the same receptor binding efficiency and potency as full-length kisspeptin. Kisspeptin-14 human binds to its receptor GPR54 and is able to activate this G protein-coupled receptor and activate multiple intracellular signaling pathways. Kisspeptin-14 human can be used to study reproductive development and tumor metastasis .

Cat. No.	Product Name		Classification

HY-112766

DPyPE		Phospholipids
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 .

HY-172699A

DSPE-PEG3400-ANG		Pegylated Lipids
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 .

HY-172700

DSPE-PEG5000-ANG		Pegylated Lipids
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 .

HY-172698

DSPE-PEG1000-ANG		Pegylated Lipids
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 .

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