1. JAK/STAT Signaling
    Stem Cell/Wnt
    Apoptosis
  2. STAT
    Apoptosis
  3. STAT3-IN-1

STAT3-IN-1 

Cat. No.: HY-100753
Handling Instructions

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.

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

STAT3-IN-1 Chemical Structure

STAT3-IN-1 Chemical Structure

CAS No. : 2059952-75-7

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Description

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis[1].

IC50 & Target

IC50: 1.82 μM (STAT3 in HT29 cells), 2.14 μM (STAT3 in MDA-MB 231 cells)[1].

In Vitro

STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions[1].
STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) induces tumor cells apoptosis in MDA-MB-231 cells[1].

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cell lines.
Concentration: 0-10 μM.
Incubation Time: 48 hours.
Result: The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 mM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and HT-29 cell lines.
Concentration: 0-10 μM.
Incubation Time: 48 hours.
Result: Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.
Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685.
In Vivo

STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model[1].

Animal Model: Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells[1].
Dosage: 10, 20 mg/kg.
Administration: Oral administration once every other day for two weeks.
Result: Arrested tumor growth with no obvious body weight loss.
Molecular Weight

475.53

Formula

C₂₈H₂₉NO₆

CAS No.

2059952-75-7

SMILES

COC1=CC(OC)=CC(/C=C/C2=CC=C(NC(/C=C/C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=C1

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

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