STAT3-IN-11 (7a)是一种STAT3选择性抑制剂，可抑制 STAT3pTyr705位点的磷酸化。STAT3-IN-11 可抑制下游基因(Survivin 和 Mcl-1)的磷酸化，且不影响上游酪氨酸激酶 (Src and JAK2) 和 p-STAT1 的表达。STAT3-IN-11 可诱导癌细胞凋亡，有望用于 STAT3 抑制剂和抗肿瘤试剂的发现。

STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes ( Survivin and Mcl-1 ) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers [1].

STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells [1]. STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC 50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC 50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-1) [1]. STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the phosphorylation of STAT3 (stimulated by IL-6 in MDA-MB-231) at site pTyr705 in a concentration-dependent manner [1]. STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the expression of the downstream gene (Survivin and Mcl-1) of STAT3 in a concentration-dependent manner [1]. STAT3-IN-11 (2.5-10 μM, 6 h) has no effects on the typical upstream kinases of STAT3 such as p-JAK2 and p-Src and the phosphorylation of STAT1 (a STAT isoform) [1]. STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner [1]. Cell Cytotoxicity Assay [1] Cell Line: MDA-MB-231 cells Concentration: 20 μM Incubation Time: 48 hours Result: The antiproliferative activity reached 97.86%. Cell Cytotoxicity Assay [1] Cell Line: MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells Concentration: 20 μM Incubation Time: 48 hours Result: Inhibited with IC 50 values of 6.01, 7.20, 7.02, 26.54, 25.69 and 12.52 μM for MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells, respectively. Western Blot Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 2.5,5 and 10 μM Incubation Time: 6 hours Result: Decrease the level of p-STAT3 at site pTyr705 in a concentration dependent manner. Western Blot Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 2.5,5 and 10 μM Incubation Time: 6 hours Result: Down-regulated the level of STAT3 downstream genes. Apoptosis Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 5, 10 and 15 μM Incubation Time: 48 hours Result: The percentage of apoptotic cells was 24.4% at a concentration of 15 μM.

2503096-50-0

C20H17NO4

335.35

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years