Stattic

Research use only, not for human use.

Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1.

Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1.(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.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.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.Stattic (2.5, 5, 10 μM; for 48 h) shows significant S phase accumulation.Stattic can not lead to significant morphological changes or apoptosis and has little STAT3 phosphorylation in A2780 cells and HUVECs.(In Vivo):Stattic (10 mg/kg; i.p.; three times per week for 10 week) ameliorates the renal dysfunction in Alport syndrome (AS) mice.

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Animal Model:Age-matched wild-type (WT) C57BL/6 miceDosage:10 mg/kg Administration:IP; three timesper week for 10 week Result:Increased levels of proteinuria, BUN and serum creatinine.Significantly suppressed the gene expression levels of renal injury markers (Lcn2, Kim-1), pro-inflammatory cytokines (Il-6, KC), pro-fibrotic genes (Tgf-β, Col1a1, α-Sma) and Mmp9.

STAT3 Inhibitor V

JAK/STAT Signaling

STAT

STAT3

Cancer

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19983-44-9

211.19

C8H5NO4S

>98% (HPLC)

DMSO: 42 mg/mL (198.87 mM)

O=[N+](C1=CC=C(C2=C1)C=CS2(=O)=O)[O-]

6-Nitro-1-benzothiophene 1,1-dioxide

(-20℃)

With Ice Pack

≥ 2 years