STAT3-IN-10

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STAT3-IN-10 is a STAT3 inhibitor with an IC₅₀ value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, induces cancer cells apoptosis.

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STAT3-IN-10 Chemical Structure

CAS No. : 2499491-04-0

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Description

STAT3-IN-10 is a STAT3 inhibitor with an IC₅₀ value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, induces cancer cells apoptosis^[1].

IC₅₀ & Target

STAT3

5.18 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	1.24 μM Compound: A11	Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 32603980]
MDA-MB-231	IC₅₀	0.67 μM Compound: A11	Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 32603980]
MDA-MB-468	IC₅₀	0.77 μM Compound: A11	Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 32603980]

In Vitro

STAT3-IN-10 (A11) (48 h) shows IC₅₀ values of 0.67, 0.77, 1.24 µM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively^[1].
STAT3-IN-10 (A11) directly binds to the STAT3 SH2 domain ^[1].
STAT3-IN-10 (A11) (0-3 μM, 24 h) inhibits the phosphorylation of STAT3 and its downstream target proteins and has a good selectivity against the tumor suppressor STAT1 ^[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) induces apoptosis in cancer cells^[1].
STAT3-IN-10 (A11) (0-4 μM, 24 h) dose-dependently causes a significant S phase arrest in MDA-MB-231 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2.
Concentration:
Incubation Time:	48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2).
Result:	Showed IC₅₀ values of 0.67, 0.77, 1.24 µM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231.
Concentration:	0, 0.75, 1.5 and 3.0 μM.
Incubation Time:	24 h.
Result:	Decreased the STAT3-Y705 phosphorylation without affecting the total amount of STAT3 protein and decreased the expression of STAT3 target genes, including C-Myc and Cyclin D1 in a dose-dependent manner. Had little impact on the level of STAT1 and its phosphorylation on Tyr701.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231.
Concentration:	0, 1, 2, and 4 μM.
Incubation Time:	24 h.
Result:	Induced the apoptosis in MDA-MB-231 cells in a concentration-dependent manner

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-231.
Concentration:	0, 1, 2, and 4 μM.
Incubation Time:	24 h.
Result:	Could dose-dependently cause a significant S phase arrest in MDA-MB-231 cells

In Vivo

STAT3-IN-10 (A11) (i.p.; 5, 10 mg/kg; once a day, 21 days) inhibits the growth of human xenograft tumor in vivo^[1].

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

Animal Model:	Five weeks old female BALB/c nude mice (16–18g) bearing inoculation of human breast cancer cells MDA-MB-231^[1].
Dosage:	5 and 10 mg/kg
Administration:	IP, once a day, 21 days
Result:	Inhibited the growth of human xenograft tumor in vivo without apparent body-weight loss for treated mice and inhibited the levels of p-STAT3 in tumor tissues.

Molecular Weight

311.29

Formula

C₁₇H₁₃NO₅

CAS No.

2499491-04-0

SMILES

COC(C=C1)=CC=C1NC2=CC(C3=C(C2=O)OC(C(C)=O)=C3)=O

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]. Kai-Rui Feng, et al. Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy. Eur J Med Chem. 2020 Sep 1;201:112428. [Content Brief]

STAT3-IN-10 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-102499491-04-0STATApoptosisMDA-MB-231HepG2antitumorInhibitorinhibitorinhibit

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