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

STAT3-IN-1 

Cat. No.: HY-100753 Purity: 96.54%
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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100 mg USD 980 In-stock
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Based on 1 publication(s) in Google Scholar

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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[1]

Stat-3

1.82 μM (IC50, in HT29 cells)

Stat-3

2.14 μM (IC50, in MDA-MB 231 cells)

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 μM 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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (262.86 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1029 mL 10.5146 mL 21.0292 mL
5 mM 0.4206 mL 2.1029 mL 4.2058 mL
10 mM 0.2103 mL 1.0515 mL 2.1029 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 6.25 mg/mL (13.14 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

STAT3-IN-1STATApoptosisInhibitorinhibitorinhibit

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STAT3-IN-1
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HY-100753
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