2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. STAT3-IN-3

STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.

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STAT3-IN-3 Chemical Structure

STAT3-IN-3 Chemical Structure

CAS No. : 2361304-26-7

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Based on 4 publication(s) in Google Scholar

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Description

STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research[1].

IC50 & Target[1]

STAT3

 

In Vitro

STAT3-IN-3 has no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2[1].
STAT3-IN-3 inhibits the growth of MDA-MB-231, HCT-116, HepG2, and MCF-7 cells with IC50s of 1.43 μM, 1.89 μM, 2.88 μM, and 3.33 μM, respectively[1].
STAT3-IN-3 down-regulates the expression of STAT3 target genes Bcl-2 and Cyclin D1[1].
STAT3-IN-3 inhibits STAT3 tyrosine phosphorylation and serine phosphorylation[1].
STAT3-IN-3 inhibits STAT3 DNA-binding activity[1].
STAT3-IN-3 (1-4 μM; 24 hours) increases ROS production and remarkably reduces the mitochondrial membrane potential to induce mitochondrial apoptotic pathway[1].
STAT3-IN-3 (1-4 μM; 24 hours) can induce the cleavage of caspase-9, caspase-3 and PARP[1].

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

STAT3-IN-3 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells, HCT-116 cells, HepG2 cells, MCF-7cells
Concentration: MTT assay
Incubation Time: 48 hours
Result: Exhibited anti-proliferative activity.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Induced the apoptosis of MDA-MB-231 cells dose-dependently and the apoptosis rates.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 24 hours
Result: Induced the cleavage of caspase-9, caspase-3 and PARP.
In Vivo

STAT3-IN-3 (10mg/kg-20 mg/kg; i.p.; daily; for 14 days) possesses potent antitumor activity against implanted 4T1 breast tumors growth[1].

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

Animal Model: Adult female BALB/c mice (6 weeks of age)[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection, daily, for 14 days
Result: Significantly inhibited tumor volume.
Molecular Weight

600.48

Formula

C27H26BrN3O6S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

BrC1=C2C(S(C(C(N3CCN(C(C4=CC5=CC=C(N(CC)CC)C=C5OC4=O)=O)CC3)=O)=C2)(=O)=O)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (8.33 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 1.6653 mL 8.3267 mL 16.6533 mL
5 mM 0.3331 mL 1.6653 mL 3.3307 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6653 mL 8.3267 mL 16.6533 mL 41.6334 mL
5 mM 0.3331 mL 1.6653 mL 3.3307 mL 8.3267 mL
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STAT3-IN-3 Related Classifications

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-32361304-26-7STATApoptosisSTAT3mitochondria-targetingantitumormitochondrialapoptosispathwayInhibitorinhibitorinhibit

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