STAT3-IN-11

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

STAT3-IN-11 (7a)是一种STAT3 选择性抑制剂，可抑制 STAT3 pTyr705 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.

STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells.STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-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 dose-dependent manner.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.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) .STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner.Cell Cytotoxicity Assay Cell Line:MDA-MB-231 cells Concentration:20 μM Incubation Time:48 hours Result:The antiproliferative activity reached 97.86%.Cell Cytotoxicity Assay Cell Line:MDA-MB231, A549, MDA-MB-10A, PBMCs and HFL-1 cells Concentration:20 μM Incubation Time:48 hours Result:Inhibited with IC50 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 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 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 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.

——

——

Apoptosis

Apoptosis

Apoptosis | STAT

——

——

2503096-50-0

335.35

C20H17NO4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (298.20 mM; 超声助溶 )

CC1=C(CCNC(=O)c2ccccc2)C(=O)c2c(O)cccc2C1=O

——

(-20℃)

With Ice Pack

≥ 2 years