STAT3-IN-14

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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

CAS No. : 123297-90-5

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References
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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.

123297-90-5

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

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Teruyuki Tahara, et al. STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae. Bioorg Med Chem. 2020 Mar 15;28(6):115347. [Content Brief]

STAT3-IN-14 Related Classifications

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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.

Keywords:

STAT3-IN-14123297-90-5STATSTAT3 inhibitorJAK/STAT pathwayMDA-MB-231MCF7 A549Inhibitorinhibitorinhibit

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