2. JAK/STAT Signaling Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis
  3. STAT CDK c-Myc Apoptosis
  4. STAT3-IN-53

STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer.

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

STAT3-IN-53

STAT3-IN-53 Chemical Structure

CAS No. : 3113051-34-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

STAT3-IN-53 Related Antibodies

Top Publications Citing Use of Products

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer[1].

IC50 & Target[1]

STAT3

6.16 μM (Kd)

In Vitro

STAT3-IN-53 directly binds to recombinant full-length wild-type STAT3 protein with a Kd of 6.16 μM[1].
STAT3-IN-53 (concentration gradient) potently inhibits the IL-6/JAK/STAT3 signaling pathway in HEK-BLUE-IL6 cells with an IC50 of 0.89 ± 0.07 μM[1].
STAT3-IN-53 (concentration gradient; 96 h) potently inhibits the proliferation of HCT116, HT29, SW480, MC38, and CT26 colorectal cancer cell lines, with the highest activity in HCT116 cells (IC50 = 0.45 ± 0.05 μM)[1].

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

STAT3-IN-53 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT116, HT29, SW480, MC38, CT26 colorectal cancer cell lines
Concentration: concentration gradient (for IC50 determination)
Incubation Time: 96 h
Result: Exhibited potent antiproliferative activity across all tested colorectal cancer cell lines, with IC50 values of 0.45 ± 0.05 μM (HCT116), 1.80 ± 0.10 μM (HT29), 9.34 ± 0.79 μM (SW480), 2.33 ± 0.48 μM (MC38), and 5.14 ± 0.84 μM (CT26).

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.5, 2.5 μM
Incubation Time: 24 h
Result: Dose-dependently suppressed STAT3 phosphorylation at the Y705 residue without altering total STAT3 protein levels.
Did not inhibit phosphorylation of STAT6 or SRC.
Dose-dependently downregulated cyclin-D1 expression.
In Vivo

STAT3-IN-53 (5-20 mg/kg; i.p.; once daily; 12 days) exerts a dose-dependent inhibitory effect on the growth of subcutaneous MC38 colon adenocarcinoma in C57BL/6J mice[1].

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

Animal Model: C57BL/6J (male, SPF grade, 18-20 g, subcutaneous implantation of MC38 colon adenocarcinoma tumor fragments)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.p.; once daily; 12 days
Result: Achieved a tumor growth inhibition (TGI) rate of 53.6% at 5 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 59.8% at 20 mg/kg.
Suppressed STAT3 Y705 phosphorylation in tumor tissues at 20 mg/kg.
Downregulated Cyclin-D1 and c-Myc protein expression in tumor tissues at 20 mg/kg.
Caused no treatment-related adverse events or body weight loss exceeding 10% during the 12-day dosing period.
Molecular Weight

678.73

Formula

C33H33F3N8O3S
CAS No.
SMILES

O=C(OCC)C1=NC=CC(C2=NN=C(NC3=C(N4CCN(CC)CC4)C=C5N(C6CC6)C(C7=CC=C(OC(F)(F)F)C=C7)=NC5=C3)S2)=C1
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

STAT3-IN-53 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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-533113051-34-3STATCDKc-MycApoptosisCyclin dependent kinaseMycmurine subcutaneous xenograft modelIL-6/JAK/STAT3 pathwayY705SH2 domaincolorectal cancer cellsSTAT3HEK-BLUE-IL6 cellsHCT116 cellscyclin-D1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
STAT3-IN-53
Cat. No.:
HY-181514
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.