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.

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

STAT3-IN-3 Chemical Structure

STAT3-IN-3 Chemical Structure

CAS No. : 2361304-26-7

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Based on 6 publication(s) in Google Scholar

STAT3-IN-3 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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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

 

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
1.89 μM
Compound: 7a
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31048139]
HepG2 IC50
2.88 μM
Compound: 7a
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31048139]
L02 IC50
35.6 μM
Compound: 7a
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31048139]
MCF-10A IC50
14.62 μM
Compound: 7a
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF10A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31048139]
MCF7 IC50
3.33 μM
Compound: 7a
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31048139]
MDA-MB-231 IC50
1.43 μM
Compound: 7a
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31048139]
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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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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