Stattic

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]. 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].