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AQP1 Inhibitors

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By Targets:	Aquaporin (5) Akt (2) Apoptosis (4) Cadherin (1) Caspase (1) Drug Metabolite (1) Monoamine Oxidase (2) PI3K (2) PKC (2) Pregnane X Receptor (PXR) (2) Reference Standards (2) TGF-beta/Smad (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Endocrinology (1) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Targets Recommended: Aquaporin Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N2013

Aristolactam I 1 Publications Verification Aristololactam; Aristolactam	Drug Metabolite Aquaporin Cadherin TGF-beta/Smad	Endocrinology Cancer
Aristolactam I is an *AQP1* inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .

HY-N6016

Bacopaside II 1 Publications Verification	Apoptosis Aquaporin	Cancer
Bacopaside II, an extract from the medicinal herb Bacopa monnieri. Bacopaside II is the inhibitor for *AQP1* that exhibits anti-angiogenesis activity. Bacopaside II exhibits cytotoxicity and induces apoptosis in cancer cells .

HY-N4246

Bacopaside I	Aquaporin PKC Akt PI3K Apoptosis Monoamine Oxidase Pregnane X Receptor (PXR)	Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
Bacopaside I is an orally active aquaporin *AQP1* inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of *AQP1* without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .

HY-110200

TC AQP1 1 2 Publications Verification m-Phenylenediacrylic acid; m-Benzenediacrylic acid	Aquaporin	Metabolic Disease Cancer
TC AQP1 1 (m-Phenylenediacrylic acid) is a potent *AQP1* inhibitor. TC AQP1 1 inhibits AQP1-mediated water flux in oocytes, with an IC₅₀ of 8 μM .

HY-N4246R

Bacopaside I (Standard)	Reference Standards PKC Akt PI3K Apoptosis Pregnane X Receptor (PXR) Monoamine Oxidase Aquaporin	Neurological Disease
Bacopaside I (Standard) is the analytical standard of Bacopaside I. This product is intended for research and analytical applications. Bacopaside I is an orally active aquaporin *AQP1* inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of *AQP1* without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .

HY-N2013R

Aristolactam I (Standard) Aristololactam (Standard); Aristolactam (Standard)	Reference Standards Caspase Apoptosis	Inflammation/Immunology
Aristolactam I (Standard) is the analytical standard of Aristolactam I. This product is intended for research and analytical applications. Aristolactam I is an *AQP1* inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2013

Aristolactam I 1 Publications Verification Aristololactam; Aristolactam	Structural Classification Natural Products other families Classification of Application Fields Plants Inflammation/Immunology Disease Research Fields Source Classification	Drug Metabolite Aquaporin Cadherin TGF-beta/Smad
Aristolactam I is an *AQP1* inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .

HY-N6016

Bacopaside II 1 Publications Verification	Triterpenes Classification of Application Fields Terpenoids Scrophulariaceae Plants Disease Research Fields Bacopa monnieri (Linn.) Wettst. Source Classification Cancer	Apoptosis Aquaporin
Bacopaside II, an extract from the medicinal herb Bacopa monnieri. Bacopaside II is the inhibitor for *AQP1* that exhibits anti-angiogenesis activity. Bacopaside II exhibits cytotoxicity and induces apoptosis in cancer cells .

HY-N4246

Bacopaside I	Triterpenes Structural Classification Terpenoids Scrophulariaceae Plants Bacopa monnieri (Linn.) Wettst. Source Classification	Aquaporin PKC Akt PI3K Apoptosis Monoamine Oxidase Pregnane X Receptor (PXR)
Bacopaside I is an orally active aquaporin *AQP1* inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of *AQP1* without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .

HY-N4246R

Bacopaside I (Standard)	Triterpenes Structural Classification Terpenoids Scrophulariaceae Plants Bacopa monnieri (Linn.) Wettst. Source Classification	Reference Standards PKC Akt PI3K Apoptosis Pregnane X Receptor (PXR) Monoamine Oxidase Aquaporin
Bacopaside I (Standard) is the analytical standard of Bacopaside I. This product is intended for research and analytical applications. Bacopaside I is an orally active aquaporin *AQP1* inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of *AQP1* without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .

HY-N2013R

Aristolactam I (Standard) Aristololactam (Standard); Aristolactam (Standard)	Natural Products other families Plants Source Classification	Reference Standards Caspase Apoptosis
Aristolactam I (Standard) is the analytical standard of Aristolactam I. This product is intended for research and analytical applications. Aristolactam I is an *AQP1* inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .

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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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AQP1 Inhibitors

Inhibitors & Agonists

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