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抑制劑描述：

產(chǎn)品名稱：S3I-201

產(chǎn)品別名：2-羥基-4-[[2-[[(4-甲基苯基)磺酰基]氧基]乙?；鵠氨基]苯甲酸

英文別名：S3I201;NSC74859;NSC 74859;NSC-74859;S3I 201

靶點(diǎn)：STAT3

CAS：501919-59-1

純度：>98%

外觀：white to beige Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：

S3I-201 (NSC 74859) is a Stat3 inhibitor with IC50 of 86 μM.

溶解性：DMSO ：36.5 mg/mL (100 mM)

體外研究：

S3I-201選擇性抑制Stat3 DNA結(jié)合活性。S3I-201抑制Stat3·Stat3復(fù)合形式,不依賴于Stat3的激活狀態(tài)。S3I-201不干涉Lck SH2與同源pTyr肽結(jié)合。S3I-201作用于NIH 3T3/v-Src鼠成纖維細(xì)胞和人類乳腺癌MDA-MB-231, MDA-MB-435, 和MDA-MB-468 細(xì)胞，可以抑制Stat3激活。S3I-201 抑制Stat3依賴的轉(zhuǎn)錄活性。 S3I-201 也抑制編碼cyclin D1, Bcl-xL,和surviving 的Stat3-調(diào)節(jié)基因的表達(dá)。S3I-201可以降低 pS727STAT3水平和降低TGF-β通路蛋白水平。S3I-201也可抑制CD133+ 和CD133− Huh-7細(xì)胞。最新研究顯示S3I-201作用于Hep-G2, Huh-7和SK-HEP-1細(xì)胞，加強(qiáng) Cetuximab的抗增殖效果。

體內(nèi)研究：Human breast (MDA-MB-231) tumor-bearing mice are given an i.v. injection of NSC 74859 (S3I-201) or vehicle every 2 or every 3 days for 2 weeks, and tumor measurements are taken every 2-3 days. Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received S3I-201 display strong growth inhibition. Continued evaluation of treated mice on termination of treatment shows no resumption of tumor growth, suggesting potentially a long-lasting effect of S3I-201 on tumor growth. Compared with vehicle-treated control tumors (n=15), which continued to grow, S3I-201 treatment of somatotroph tumor xenografts (n=15) significantly attenuated tumor growth for the duration of the experiment. Tumors derived from NSC 74859-treated rats are significantly smaller than those from the untreated group (220±16 mm3 vs. 287±16 mm3, P3 vs. 708±83 mm3, P.

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