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STAT3-IN-10

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.

For research use only. We do not sell to patients.

CAS No.: 2499491-04-0
Formula: C₁₇H₁₃NO₅
Molecular Weight:311.29

Storage:

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

Data Sheet (273 KB)

STAT3-IN-10 Chemical Structure

CAS No.: 2499491-04-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

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)

All STAT Isoforms :

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.

Chemical Information

CAS No. 2499491-04-0
Molecular Weight 311.29
Formula C₁₇H₁₃NO₅
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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