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STAT3-IN-11
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
STAT3-IN-11图片
CAS NO:2503096-50-0
包装与价格：
包装价格(元)
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产品介绍
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。
生物活性

STAT3-IN-11 (7a) is a selectiveSTAT3inhibitor that inhibits the phosphorylation ofSTAT3at sitepTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (SurvivinandMcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can inducecancercellapoptosis, which is potential for the discovery of effectiveSTAT3inhibitors and antitumor agents against cancers[1].

IC50& Target

IC50: 1.93 μM (SIP), ≥ 30 μM (SphK1), ≈ 30 μM (SphK2)[1].

体外研究
(In Vitro)

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 withIC50values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50values 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 dose-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 withIC50values 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.
分子量

335.35

性状

Solid

Formula

C20H17NO4

CAS 号

2503096-50-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month