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fibrotic remodeling

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By Targets:	5-HT Receptor (2) Apoptosis (2) Caspase (2) FGFR (2) Interleukin Related (1) MMP (1) p38 MAPK (2) SARS-CoV (1) TGF-β Receptor (2) Topoisomerase (1) VEGFR (1) Virus Protease (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (4) Infection (1) Metabolic Disease (1) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-174374

Topobexin	Topoisomerase	Cardiovascular Disease
Topobexin is a TOP2B-selective inhibitor with IC₅₀ values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .

HY-15472

PRX-08066	5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase	Cardiovascular Disease Neurological Disease Cancer
PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .

HY-172350

WEHI-P8	SARS-CoV Virus Protease Interleukin Related	Infection
WEHI-P8 is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC₅₀ of 12 nM and a K_d of 9.0 nM. WEHI-P8 reduces viral load, body weight loss, pulmonary inflammation, immune cell infiltration and pro-inflammatory mediator levels in SARS-CoV-2-infected mice. WEHI-P8 prevents pulmonary hemorrhage, immune cell infiltration, fibrotic remodeling and neuroinflammation, and improves cognitive function in a mouse model of post-acute sequelae of SARS-CoV-2 infection (PASC). WEHI-P8 is applicable for the research of COVID-19 and PASC .

HY-15472A

PRX-08066 maleate	5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase	Cardiovascular Disease Neurological Disease Cancer
PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .

HY-180765

Colchicine-O-CO-Enyl(Me)-Enyl-Enyl(Me)-Enyl-1,3,3-trimethylcyclohex-1-ene	MMP	Metabolic Disease
Colchicine-O-CO-Enyl(Me)-Enyl-Enyl(Me)-Enyl-1,3,3-trimethylcyclohex-1-ene (compound L2) is a lipophilic colchicinoid formulation targeting hepatic stellate cells (HSC). Colchicine-O-CO-Enyl(Me)-Enyl-Enyl(Me)-Enyl-1,3,3-trimethylcyclohex-1-ene increases the levels of MMP2, MMP8 and MMP9, demonstrating the protective effect in tissue remodeling. Colchicine-O-CO-Enyl(Me)-Enyl-Enyl(Me)-Enyl-1,3,3-trimethylcyclohex-1-ene exhibits anti-fibrotic activity in CCL₄-induced liver fibrosis (LF) mouse model. Colchicine-O-CO-Enyl(Me)-Enyl-Enyl(Me)-Enyl-1,3,3-trimethylcyclohex-1-ene can be used for LF research .

HY-182306

VEGFR-2 ligand-2	VEGFR	Cardiovascular Disease
VEGFR-2 ligand-1, Sorafenib (HY-10201) derivative, is a vascular endothelial growth factor receptor 2 (VEGFR2) ligand. VEGFR-2 ligand-1 binds to the ATP-binding pocket of VEGFR2, forms hydrophobic contacts and hydrogen bonds with key binding-site residues. VEGFR-2 ligand-1 can be used for the research angiogenesis-related pathologies .

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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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fibrotic remodeling

Inhibitors & Agonists