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Results for "

hydrophobic ligands

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (1) Bcl-2 Family (1) Biochemical Assay Reagents (1) Ferroptosis (1) Fluorescent Dye (1) Glutathione Peroxidase (1) PPAR (1) PROTACs (1) ROR (1)
By Research Areas:	Cancer (2) Endocrinology (2) Inflammation/Immunology (1) Metabolic Disease (1)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Targets Recommended: Ligands for Target Protein for PROTAC Ligands for E3 Ligase Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-D1605

BODIPY FL L-Cystine	Fluorescent Dye	Others
BODIPY FL L-Cystine is a thiol-reactive, green-fluorescent dye. BODIPY FL L-Cystine can be the labeling of membrane proteins, proteins with hydrophobic binding sites, or hydrophobic ligands. (λ_ex=504 nm, λ_em=511 nm) .

HY-120210

XY018	ROR	Inflammation/Immunology Cancer
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC₅₀, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .

HY-W111141

BCN-OH endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne	Biochemical Assay Reagents	Others
BCN-OH (endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne) is a mitochondrial probe based on the lyophilic bidentate bicyclic ligand BCN and is a control reagent for BCN-TPP. The TPP group is a reactive sulfenic acid probe that targets mitochondria. BCN-TPP is known to affect mitochondrial energy, causing a sharp decrease in basal respiration, causing it to exhibit faster reaction kinetics with sulfonated proteins. BCN-OH does not contain hydrophobic triphenylphosphonium (TPP) ions. Using BCN-OH as a control allows the TPP group to be safely introduced when designing sulfenic acid traps .

HY-121900

LT175	PPAR	Metabolic Disease Endocrinology
LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC₅₀=0.22 μm; mPPARα:EC₅₀=0.26 μm; hPPARγ:EC₅₀=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .

HY-118260

Phendioxan	Adrenergic Receptor	Endocrinology
Phendioxan is a compound with binding activity at the α(1)-adrenaline receptor subtype. The facilitated membrane diffusion of phendioxan is thought to be associated with improved α(1d)-AR affinity. Docking simulations of phendioxan at biological targets supported the stoichiometric analysis and revealed the importance of polar, electrostatic, hydrophobic, and shape effects of its phenoxy terminal orthogonal substituents on ligand binding .

HY-161972

ZX782	PROTACs Glutathione Peroxidase Ferroptosis	Cancer
ZX782 is a Hty-type PROTAC targeting GPX4 and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination . ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).

HY-P5325

Bid BH3 (80-99)	Bcl-2 Family	Others
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrial membrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)

Cat. No.	Product Name

HY-L913

Tyrosine Focused Covalent Fragment Library	124 compounds
Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries. Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent drug discovery.

Tyrosine Focused Covalent Fragment Library

124 compounds

Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries.

Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent drug discovery.

Cat. No.	Product Name	Type

HY-D1605

BODIPY FL L-Cystine	Fluorescent Dyes/Probes
BODIPY FL L-Cystine is a thiol-reactive, green-fluorescent dye. BODIPY FL L-Cystine can be the labeling of membrane proteins, proteins with hydrophobic binding sites, or hydrophobic ligands. (λ_ex=504 nm, λ_em=511 nm) .

Cat. No.	Product Name	Type

HY-W111141

BCN-OH endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne	Biochemical Assay Reagents
BCN-OH (endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne) is a mitochondrial probe based on the lyophilic bidentate bicyclic ligand BCN and is a control reagent for BCN-TPP. The TPP group is a reactive sulfenic acid probe that targets mitochondria. BCN-TPP is known to affect mitochondrial energy, causing a sharp decrease in basal respiration, causing it to exhibit faster reaction kinetics with sulfonated proteins. BCN-OH does not contain hydrophobic triphenylphosphonium (TPP) ions. Using BCN-OH as a control allows the TPP group to be safely introduced when designing sulfenic acid traps .

BCN-OH

endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne

Biochemical Assay Reagents

BCN-OH (endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne) is a mitochondrial probe based on the lyophilic bidentate bicyclic ligand BCN and is a control reagent for BCN-TPP. The TPP group is a reactive sulfenic acid probe that targets mitochondria. BCN-TPP is known to affect mitochondrial energy, causing a sharp decrease in basal respiration, causing it to exhibit faster reaction kinetics with sulfonated proteins. BCN-OH does not contain hydrophobic triphenylphosphonium (TPP) ions. Using BCN-OH as a control allows the TPP group to be safely introduced when designing sulfenic acid traps .

Cat. No.	Product Name	Target	Research Area

HY-P5325

Bid BH3 (80-99)	Bcl-2 Family	Others
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrial membrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)

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