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MedChemExpressModel Stattic -19983-44-9

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Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727)[1]. Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3[2]. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].
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Stattic

MCE China:Stattic

Brand:MedChemExpress (MCE)

Cat. No.HY-13818

CAS:19983-44-9

Purity:99.58%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

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

Description:Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727). Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice.

In Vitro:Stattic (20 μM; 24 hours) inhibits STAT3 phosphorylation (Y705) and selectively inhibits P-STAT3 as demonstrated by the lack of inhibition of P-ERK1/2 in ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines[1]. Stattic (2.5, 5, 10 μM; for 4 h) significantly reduces the nuclear level of pSTAT3 and survivin in PC3M-1E8 cells at 10 μM. Stattic (2.5-10 μM; for 24 h) inhibits IL-6-induced STAT3 activation in a dose-dependent manner[2]. Stattic (2.5, 5, 10 μM; for 48 h) suppresses both the growth and induces apoptosis prostate cancer cells (PC3M-1E8 cells) with 10 μM. Stattic does not induce significant cell apoptosis with 2.5 μM, 5 μM[2]. Stattic (2.5, 5, 10 μM; for 48 h) shows significant S phase accumulation[2]. Stattic can not lead to significant morphological changes or apoptosis and has little STAT3 phosphorylation in A2780 cells and HUVECs[2].

In Vivo:Stattic (10 mg/kg; i.p.; three times per week for 10 week) ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].

IC50 & Target:STAT3

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References:

[1]. Lin L, et al. STAT3 as a potential therapeutic target in ALDH+ and CD44+/CD24+ stem cell-like pancreatic cancer cells. Int J Oncol. 2016 Oct 12.  [Content Brief]

[2]. John S McMurray, et al. A new small-molecule Stat3 inhibitor. Chem Biol. 2006 Nov;13(11):1123-4.  [Content Brief]

[3]. Tsubasa Yokota, et al. STAT3 inhibition attenuates the progressive phenotypes of Alport syndrome mouse model. Nephrol Dial Transplant. 2018 Feb 1;33(2):214-223.  [Content Brief]

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