Stattic

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Stattic 是第一个非肽类小分子，可有效抑制 STAT3 激活和核转位，IC50 为 5.1 μM，选择性高于 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