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MedChemExpress - Model Esculetin - ...

MedChemExpress - Model Esculetin - 305-01-1

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities[1].

Esculetin

MCE China：Esculetin

Brand：MedChemExpress (MCE)

Cat. No.HY-N0284

CAS：305-01-1

Purity：99.78%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

In Vitro：Esculetin (40 μM, 24 h or 48 h) inhibits PDGF-BB-induced ASMC proliferation and migration[1]. Esculetin (40 μM, 1 h) inhibits PDGF-BB-induced ECM secretion and activation of PI3K/Akt pathway in ASMC cells[1]. Esculetin (100 μM, 36 h) induces pancreatic cancer cell (such as PANC-1 cells) apoptosis and loss of mitochondrial membrane potential by activation of caspases 3, 8 and 9[2]. Esculetin (100 μM, 0-12 h) binds to KEAP1 and inhibits its interaction with Nrf2 in pancreatic cancer cells (in PANC-1 cells)[2].

In Vivo：Esculetin (50 and 100 mg/kg/day, p.o., 7d) ameliorates skin lesion in Imiquimod (HY-B0180) (IMQ)-induced psoriatic mice[3]. Esculetin (10 or 30 mg/kg, i.p., three times per week for 28 days) inhibits tumor growth and metastasis via Axin2 suppression in an HCT116-implanted orthotopic mouse model[4]. Esculetin (oral gavage, 25 mg/kg for 35 days) inhibits acute restraint stress (ARS)-induced oxidative stress in mature adult mice by increasing antioxidant enzyme activities, the GSH/GSSG ratio, and cytochrome c oxidase activity in cortex[5].

IC50 & Target：PI3K

References：

[1]. Xie C, et al. Esculetin regulates the phenotype switching of airway smooth muscle cells. Phytother Res. 2019 Aug 21. [Content Brief]

[2]. Arora R, et al. Esculetin induces antiproliferative and apoptotic response in pancreatic cancer cells by directly binding to KEAP1. Mol Cancer. 2016 Oct 18;15(1):64. [Content Brief]

[3]. Chen Y, et al. Esculetin Ameliorates Psoriasis-Like Skin Disease in Mice by Inducing CD4+Foxp3+ Regulatory T Cells. Front Immunol. 2018 Sep 12;9:2092. [Content Brief]

[4]. Kim WK, et al. Esculetin suppresses tumor growth and metastasis by targeting Axin2/E-cadherin axis in colorectal cancer. Biochem Pharmacol. 2018 Jun;152:71-83. [Content Brief]

[5]. Martín-Aragón S, et al. Age-dependent effects of esculetin on mood-related behavior and cognition from stressed mice are associated with restoring brain antioxidant status. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Feb 4;65:1-16. [Content Brief]

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