1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. STAT3-IN-14

STAT3-IN-14(Compound 1) 是一种 STAT3 抑制剂,具有 STAT3 磷酸化抑制活性,可直接与 STAT3的铰链区结合。

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STAT3-IN-14 Chemical Structure

STAT3-IN-14 Chemical Structure

CAS No. : 123297-90-5

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查看 STAT 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3[1].

IC50 & Target

IC50: 0.42 μM (MDA-MB-231); 0.50 μM (MCF7); 0.13 μM (A549) [1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.13 μM
Compound: 1
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
A549 EC50
0.78 μM
Compound: 1
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
A549 EC50
0.96 μM
Compound: 1
Cytotoxicity against human A549 cells assessed as cell viability by tryptan blue staining method
Cytotoxicity against human A549 cells assessed as cell viability by tryptan blue staining method
[PMID: 17950604]
Fibroblast EC50
11.1 μM
Compound: 1
Antiproliferative activity against human skin fibroblast after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human skin fibroblast after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
Hepatocyte EC50
11.1 μM
Compound: 1
Antiproliferative activity against human hepatocytes after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human hepatocytes after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
MCF7 IC50
0.5 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
MCF7 EC50
0.51 μM
Compound: 1
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
MCF7 IC50
2 μM
Compound: 1
Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis
Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis
[PMID: 32044231]
MCF7 EC50
3.5 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as cell viability by tryptan blue staining method
Cytotoxicity against human MCF7 cells assessed as cell viability by tryptan blue staining method
[PMID: 17950604]
MDA-MB-231 IC50
0.41 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
PC-3 EC50
0.14 μM
Compound: 1
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
PC-3 EC50
0.14 μM
Compound: 1
Cytotoxicity against human PC3 cells assessed as cell viability by tryptan blue staining method
Cytotoxicity against human PC3 cells assessed as cell viability by tryptan blue staining method
[PMID: 17950604]
Raji IC50
33.2 μM
Compound: 1
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
[PMID: 19674905]
体外研究
(In Vitro)

STAT3-IN-14 (Compound 1) shows inhibitory activity against phosphor-STAT3.
STAT3-IN-14 (Compound 1) reduces the phosphorylation inhibitory activity against MDA-MB-231 cells (JAK/STAT pathway constitutively active) in does dependent manner, but no inhibitory activities against JAK kinases.
STAT3-IN-14 (Compound 1) has growth inhibitory activity with with IC50 values of 0.42 μM, 0.50 μM and 0.13 μM in MDA-MB-231, MCF7 and A549cells, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MCF7 cells; MDA-MB-231 cells
Concentration: 1 or 10 μM; 0.5, 1, 2, 4 μM
Incubation Time: 1 h; 2 h
Result: Completely inhibited STAT3 phosphorylation at 10 μM, and partial inhibition at 1 μM.
Reduced the phosphorylation of STAT3 in does dependent manner.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MCF7 and A549 cells
Concentration: 0-30 μM
Incubation Time: 72 h
Result: Showed moderate to strong growth inhibitory activity among the three cancer cell lines.
分子量

258.23

Formula

C14H10O5

CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
STAT3-IN-14
目录号:
HY-N10472
需求量: