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competition binding

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Chloride Channel (1) Endogenous Metabolite (1) Fluorescent Dye (1) GABA Receptor (1) Insulin Receptor (2) MHC (1) RAR/RXR (1) γ-secretase (1)
By Research Areas:	Cancer (2) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Peptides

Inhibitory Antibodies

Targets Recommended: Emopamil Binding Protein Cdc42-binding kinase FKBP YB-1 Penicillin-binding protein (PBP) ATP-binding cassette (ABC) transporters FABP Oxysterol-binding Protein-related Protein (ORP) Transthyretin (TTR) Ligands for Target Protein for PROTAC SDCBP GHR P-glycoprotein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P10138

human GIP(3-30), amide 1 Publications Verification	Insulin Receptor	Metabolic Disease
Human GIP(3-30), amide is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide has potential anti-obesity and anti-diabetic effects .

HY-109520

Glatiramer acetate 2 Publications Verification	MHC	Inflammation/Immunology Cancer
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, inhibits Experimental autoimmune encephalomyelitis (EAE), and can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression .

HY-P10138A

human GIP(3-30), amide TFA 1 Publications Verification	Insulin Receptor	Metabolic Disease
Human GIP(3-30), amide TFA is the TFA salt form of human GIP(3-30), amide (HY-P10138). Human GIP(3-30), amide TFA is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide TFA has potential anti-obesity and anti-diabetic effects .

HY-D1190

DC271	RAR/RXR	Others
DC271 is a RAR agonist and synthetic retinoid that binds to the retinoid-binding site of cellular retinoic acid-binding protein II (CRBP-II). DC271 exhibits solvatochromic fluorescence properties: it produces intense blue-shifted emission in nonpolar environments and weak red-shifted emission in polar environments, and its severe fluorescence quenching in aqueous solutions can be reversed by embedding in the hydrophobic retinoid-binding protein pocket. DC271 enables direct detection of the binding between unlabeled compounds and related retinoid-binding proteins via fluorescence competition assays (Ex/Em = 355 nm/460 nm) .

HY-W015050

1-Anthramine 1-Aminoanthracene	GABA Receptor Chloride Channel Fluorescent Dye	Neurological Disease
1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with K_d = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC₅₀ value of 16 μM .

HY-118124

2-Iodoestradiol	Endogenous Metabolite	Others
2-Iodoestradiol is a potent human sex hormone binding globulin (SHBG) ligand with a remarkably high affinity for SHBG. 2-Iodoestradiol exhibits competition for the same binding site as dihydrotestosterone in binding to human SHBG. The binding affinity constant of 2-Iodoestradiol at physiological pH and 37 degrees Celsius is 2.4 x 10(9) M-1, exceeding that for SHBG. 2-Iodoestradiol has been shown to bind to serum albumin, but with lower affinity. The radioisotope 125I-derivative of 2-Iodoestradiol has been used to study the binding properties of human SHBG, demonstrating its potential application in biological research .

HY-P992275

Anti-Nicastrin Antibody (A5226A)	γ-secretase	Neurological Disease Cancer
Anti-Nicastrin Antibody (A5226A) is a monoclonal antibody against Nicastrin and an inhibitor of γ-secretase. Anti-Nicastrin Antibody (A5226A) recognizes the fully glycosylated mature presenilin enhancer in the active γ-secretase complex and inhibits its activity via competition for substrate binding. Anti-Nicastrin Antibody (A5226A) abrogates the growth of cancer cells dependent on γ-secretase activity. Anti-Nicastrin Antibody (A5226A) serves as an imaging tool to visualize the endocytic trafficking of active γ-secretase, and also acts as a detection reagent to evaluate the endocytic efficiency of γ-secretase. Anti-Nicastrin Antibody (A5226A) can be used in studies related to non-small cell lung cancer, T-cell acute lymphoblastic leukemia and Alzheimer's disease .

Cat. No.	Product Name

HY-L907

MCE Kinase Hinge Binder Fragment Library	12,417 compounds
The most prominent mechanism of action of kinase inhibitors is their competition with ATP by binding to the hinge region of the kinase protein. Once the kinase is blocked by an inhibitor, it loses the ability to transfer phosphate groups from ATP to other molecules, resulting in the loss of kinase activity. The hinge-binding region of kinase inhibitors mimics the interaction pattern between the ATP nucleobase and the kinase. MCE extracted thousands of kinase inhibitors from the ChEMBL database and isolated their molecular fragments. In certain cases, the amino and amide groups on the molecular fragments are crucial for binding in the hinge region. Therefore, we enhanced the diversity of the collected results by adding these two groups to unoccupied positions on the ring system. Subsequently, the fragments were assessed for their hinge region binding ability via docking at distinct kinases, we also applied pharmacophore constraints to ensure interactions with key amino acids in the kinase hinge region, ultimately obtaining kinase-related molecular fragments. MCE provides over 12,417 kinase fragment molecules that meet the above requirements and are available off the shelf, serving as an effective tool for screening and developing drugs targeting kinases.

MCE Kinase Hinge Binder Fragment Library

12,417 compounds

The most prominent mechanism of action of kinase inhibitors is their competition with ATP by binding to the hinge region of the kinase protein. Once the kinase is blocked by an inhibitor, it loses the ability to transfer phosphate groups from ATP to other molecules, resulting in the loss of kinase activity.

The hinge-binding region of kinase inhibitors mimics the interaction pattern between the ATP nucleobase and the kinase. MCE extracted thousands of kinase inhibitors from the ChEMBL database and isolated their molecular fragments. In certain cases, the amino and amide groups on the molecular fragments are crucial for binding in the hinge region. Therefore, we enhanced the diversity of the collected results by adding these two groups to unoccupied positions on the ring system. Subsequently, the fragments were assessed for their hinge region binding ability via docking at distinct kinases, we also applied pharmacophore constraints to ensure interactions with key amino acids in the kinase hinge region, ultimately obtaining kinase-related molecular fragments.

MCE provides over 12,417 kinase fragment molecules that meet the above requirements and are available off the shelf, serving as an effective tool for screening and developing drugs targeting kinases.

Cat. No.	Product Name	Type

HY-D1190

DC271	Fluorescent Dye
DC271 is a RAR agonist and synthetic retinoid that binds to the retinoid-binding site of cellular retinoic acid-binding protein II (CRBP-II). DC271 exhibits solvatochromic fluorescence properties: it produces intense blue-shifted emission in nonpolar environments and weak red-shifted emission in polar environments, and its severe fluorescence quenching in aqueous solutions can be reversed by embedding in the hydrophobic retinoid-binding protein pocket. DC271 enables direct detection of the binding between unlabeled compounds and related retinoid-binding proteins via fluorescence competition assays (Ex/Em = 355 nm/460 nm) .

DC271

Fluorescent Dye

DC271 is a RAR agonist and synthetic retinoid that binds to the retinoid-binding site of cellular retinoic acid-binding protein II (CRBP-II). DC271 exhibits solvatochromic fluorescence properties: it produces intense blue-shifted emission in nonpolar environments and weak red-shifted emission in polar environments, and its severe fluorescence quenching in aqueous solutions can be reversed by embedding in the hydrophobic retinoid-binding protein pocket. DC271 enables direct detection of the binding between unlabeled compounds and related retinoid-binding proteins via fluorescence competition assays (Ex/Em = 355 nm/460 nm) .

Cat. No.	Product Name	Target	Research Area

HY-P10138

human GIP(3-30), amide 1 Publications Verification	Insulin Receptor	Metabolic Disease
Human GIP(3-30), amide is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide has potential anti-obesity and anti-diabetic effects .

HY-P10138A

human GIP(3-30), amide TFA 1 Publications Verification	Insulin Receptor	Metabolic Disease
Human GIP(3-30), amide TFA is the TFA salt form of human GIP(3-30), amide (HY-P10138). Human GIP(3-30), amide TFA is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide TFA has potential anti-obesity and anti-diabetic effects .

Cat. No.	Product Name	Target	Research Area	Image

HY-P992275

Anti-Nicastrin Antibody (A5226A)	γ-secretase	Neurological Disease Cancer
Anti-Nicastrin Antibody (A5226A) is a monoclonal antibody against Nicastrin and an inhibitor of γ-secretase. Anti-Nicastrin Antibody (A5226A) recognizes the fully glycosylated mature presenilin enhancer in the active γ-secretase complex and inhibits its activity via competition for substrate binding. Anti-Nicastrin Antibody (A5226A) abrogates the growth of cancer cells dependent on γ-secretase activity. Anti-Nicastrin Antibody (A5226A) serves as an imaging tool to visualize the endocytic trafficking of active γ-secretase, and also acts as a detection reagent to evaluate the endocytic efficiency of γ-secretase. Anti-Nicastrin Antibody (A5226A) can be used in studies related to non-small cell lung cancer, T-cell acute lymphoblastic leukemia and Alzheimer's disease .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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