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GATOR2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (12) mTOR (2) Reference Standards (2)
By Research Areas:	Cancer (4) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (14)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100228A

SKF89976A hydrochloride d,l-SKF89976A hydrochloride	GABA Receptor	Neurological Disease
SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC₅₀s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-100809

Guvacine hydrochloride 1 Publications Verification	GABA Receptor	Neurological Disease
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC₅₀s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

HY-N2482A

Guvacine hydrobromide 1 Publications Verification	GABA Receptor	Neurological Disease
Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC₅₀ values of 39 μM, 58 μM and 378 μM, respectively .

HY-103534

CI-966 hydrochloride	GABA Receptor	Neurological Disease
CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities ^[2] .

HY-119591

BPDBA	GABA Receptor	Neurological Disease
BPDBA is a selective and noncompetitive betaine/GABA transporter (BGT-1) inhibitor with IC₅₀s of 20 μM and 35 μM against human BGT-1 and mouse GAT2, respectively .

HY-N2482

Guvacine	GABA Receptor	Neurological Disease
Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC₅₀ values of 39 μM, 58 μM and 378 μM, respectively .

HY-W073239

(R)-2-Amino-5,5,5-trifluoropentanoic acid		Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
(R)-2-Amino-5,5,5-trifluoropentanoic acid is a leucine antagonist. (R)-2-Amino-5,5,5-trifluoropentanoic acid increases *Sestrin2* binding to *GATOR2. (R)-2-Amino-5,5,5-trifluoropentanoic* acid can be used in research on diabetes, neurodegenerative diseases, immune diseases, and cancer .

HY-W078733

(S)-2-Amino-4,4,4-trifluorobutanoic acid (2S)-2-Amino-4,4,4-trifluorobutanoic acid	mTOR	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
(S)-2-Amino-4,4,4-trifluorobutanoic acid ((2S)-2-Amino-4,4,4-trifluorobutanoic acid) is a *Sestrin-GATOR2* modulator. (S)-2-Amino-4,4,4-trifluorobutanoic acid can be used in research on diabetes, neurodegenerative diseases, immune diseases, and cancer .

HY-100228

SKF 89976A	GABA Receptor	Neurological Disease
SKF89976A is a selective GABA transporter (GAT-1) inhibitor with IC₅₀s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-W074912

(S)-2-Amino-5,5,5-trifluoropentanoic acid (S)-5,5,5-Trifluoronorvaline; H-Nva(5,5,5-triF)-OH	mTOR	Neurological Disease Metabolic Disease Cancer
(S)-2-Amino-5,5,5-trifluoropentanoic acid ((S)-5,5,5-Trifluoronorvaline; H-Nva (5,5,5-triF)-OH) is a selective *Sestrin-GATOR2* modulator that indirectly inhibits mTORC1 activity via a competitive binding mechanism. (S)-2-Amino-5,5,5-trifluoropentanoic acid can be used in research on cancer, metabolic diseases, neurodegenerative diseases, and muscle atrophy .\n

HY-123240

CI-966	GABA Receptor	Neurological Disease
CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities ^[2] .

HY-118207

LU-32-176B	GABA Receptor	Cancer
LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC₅₀ values of 2μM, 1μM, 4μM, respectively ^[2].

HY-100228AR

SKF89976A hydrochloride (Standard) d,l-SKF89976A hydrochloride (Standard)	GABA Receptor Reference Standards	Neurological Disease
SKF89976A (hydrochloride) (Standard) is the analytical standard of SKF89976A (hydrochloride) (HY-100228A). This product is intended for research and analytical applications. SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-182944

GATT-44	GABA Receptor	Neurological Disease
GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC₅₀ of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated ¹⁸F-radiofluorination. The radiolabeled GATT-44 ([ ¹⁸F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases .

HY-103534R

CI-966 hydrochloride (Standard)	Reference Standards GABA Receptor	Neurological Disease
CI-966 hydrochloride (Standard) is the analytical standard of CI-966 hydrochloride (HY-103534). This product is intended for research and analytical applications. CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities ^[2] .

Guvacine hydrochloride 1 Publications Verification	Alkaloids Neurological Disease Classification of Application Fields Areca catechu L. Pyridine Alkaloids Palmae Plants Disease Research Fields Source Classification	GABA Receptor
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC₅₀s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

Guvacine	Alkaloids Areca catechu L. Pyridine Alkaloids Plants Palmae Source Classification	GABA Receptor
Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC₅₀ values of 39 μM, 58 μM and 378 μM, respectively .

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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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GATOR2

Inhibitors & Agonists

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