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GABA binding site

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (10) Chloride Channel (2) Fluorescent Dye (1) Insecticide (1)
By Research Areas:	Cancer (1) Infection (1) Neurological Disease (9)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Targets Recommended: GABA Receptor Emopamil Binding Protein Cdc42-binding kinase BMI1 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-120051

Afizagabar 2 Publications Verification S44819; Egis-13529	GABA Receptor	Neurological Disease
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC₅₀ of 585 nM for α5β2γ2 and a K_i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .

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-147736

GABAA receptor agonist 2	GABA Receptor	Neurological Disease
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .

HY-129927

Thiomuscimol	GABA Receptor	Others
Thiomuscimol is a GABAA receptor agonist (IC₅₀=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.

HY-108035

(-)-JM-1232 MR04A3	GABA Receptor	Neurological Disease
(-)-JM-1232 (MR04A3) targets GABA _A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA _A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI₅₀ values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia .

HY-147735

GABAA receptor agonist 1	GABA Receptor	Neurological Disease
GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .

HY-129090

CGS-9895	GABA Receptor	Neurological Disease
CGS-9895 is a *GABA* antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors .

HY-169651

GABA-IN-4	GABA Receptor	Neurological Disease
GABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABA_A receptor complex) with K_i value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents .

HY-114811

Leptophos oxon	Insecticide GABA Receptor Chloride Channel	Infection Neurological Disease
Leptophos oxon, a metabolite of leptophos, is a GABA_A receptor chloride channel inhibitor with an IC₅₀ values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABA_A receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease .

HY-P992360

GT-002	GABA Receptor	Neurological Disease Cancer
GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency .

Cat. No.	Product Name

HY-L166

Ion Channel Compound Library	1,679 compounds
Ion channel is a membrane-binding enzyme whose catalytic site is an ion conduction pore, which is opened and closed in response to specific environmental stimuli (voltage, ligand concentration, membrane tension, temperature, etc.). Ion channel provide pores for the passive diffusion of ions on the biofilm. Due to their high selectivity for ion, ion channel are generally classified as sodium (Na⁺ ), potassium (K⁺ ), calcium (Ca²⁺ ), chloride (Cl^- ), and non-specific cation channel. Ion channel is an important contributor to cell signal transduction and homeostasis. In addition to electrical signal transduction, ion channel also have many functions: regulating vascular smooth muscle contraction, maintaining normal cell volume, regulating glandular secretion, protein kinase activation, etc. Therefore, dysfunction of ion channel can lead to many diseases, and its mechanism research is particularly important. MCE designs a unique collection of 1,679 small molecules related to ion channel, mainly targeting Na⁺ channel, K⁺ channel, Ca²⁺ channel, GABA receptor, iGluR, etc. It is an essential tool for research of cardiovascular diseases, Nervous system diseases and other diseases.

Ion Channel Compound Library

1,679 compounds

Ion channel is a membrane-binding enzyme whose catalytic site is an ion conduction pore, which is opened and closed in response to specific environmental stimuli (voltage, ligand concentration, membrane tension, temperature, etc.). Ion channel provide pores for the passive diffusion of ions on the biofilm. Due to their high selectivity for ion, ion channel are generally classified as sodium (Na⁺ ), potassium (K⁺ ), calcium (Ca²⁺ ), chloride (Cl^- ), and non-specific cation channel. Ion channel is an important contributor to cell signal transduction and homeostasis. In addition to electrical signal transduction, ion channel also have many functions: regulating vascular smooth muscle contraction, maintaining normal cell volume, regulating glandular secretion, protein kinase activation, etc. Therefore, dysfunction of ion channel can lead to many diseases, and its mechanism research is particularly important.

MCE designs a unique collection of 1,679 small molecules related to ion channel, mainly targeting Na⁺ channel, K⁺ channel, Ca²⁺ channel, GABA receptor, iGluR, etc. It is an essential tool for research of cardiovascular diseases, Nervous system diseases and other diseases.

Cat. No.	Product Name	Target	Research Area	Image

HY-P992360

GT-002	GABA Receptor	Neurological Disease Cancer
GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency .

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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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