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

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.

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STAT3-IN-14 Chemical Structure

STAT3-IN-14 Chemical Structure

CAS No. : 123297-90-5

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Based on 1 publication(s) in Google Scholar

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Description

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]

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]
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].

MedChemExpress (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.
Molecular Weight

258.23

Formula

C14H10O5

CAS No.
Appearance

Solid

Color

Light brown to yellow

SMILES

O=C(C1=C2OC([C@@H](O)C)=C1)C3=C(C2=O)C=CC=C3O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (464.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8725 mL 19.3626 mL 38.7252 mL
5 mM 0.7745 mL 3.8725 mL 7.7450 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8725 mL 19.3626 mL 38.7252 mL 96.8129 mL
5 mM 0.7745 mL 3.8725 mL 7.7450 mL 19.3626 mL
10 mM 0.3873 mL 1.9363 mL 3.8725 mL 9.6813 mL
15 mM 0.2582 mL 1.2908 mL 2.5817 mL 6.4542 mL
20 mM 0.1936 mL 0.9681 mL 1.9363 mL 4.8406 mL
25 mM 0.1549 mL 0.7745 mL 1.5490 mL 3.8725 mL
30 mM 0.1291 mL 0.6454 mL 1.2908 mL 3.2271 mL
40 mM 0.0968 mL 0.4841 mL 0.9681 mL 2.4203 mL
50 mM 0.0775 mL 0.3873 mL 0.7745 mL 1.9363 mL
60 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6135 mL
80 mM 0.0484 mL 0.2420 mL 0.4841 mL 1.2102 mL
100 mM 0.0387 mL 0.1936 mL 0.3873 mL 0.9681 mL
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  • 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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Product Name:
STAT3-IN-14
Cat. No.:
HY-N10472
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