1. Apoptosis Stem Cell/Wnt JAK/STAT Signaling
  2. Apoptosis STAT
  3. STAT3-IN-9

STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase.

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STAT3-IN-9

STAT3-IN-9 Chemical Structure

CAS No. : 2987726-27-0

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Description

STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase[1].

IC50 & Target

STAT3

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
5.73 μM
Compound: C6
Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
[PMID: 33126089]
HCT-116 IC50
> 25 μM
Compound: C6
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
[PMID: 33126089]
HepG2 IC50
1.63 μM
Compound: C6
Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
[PMID: 33126089]
MDA-MB-231 IC50
5.8 μM
Compound: C6
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
[PMID: 33126089]
MDA-MB-468 IC50
0.16 μM
Compound: C6
Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
[PMID: 33126089]
U-251 IC50
> 25 μM
Compound: C6
Antiproliferative activity against human U-251 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
Antiproliferative activity against human U-251 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
[PMID: 33126089]
In Vitro

STAT3-IN-9 (compound C6) (48 h) shows potent in vitro anti-tumor activity with IC50s of 0.16, 5.80, 1.63, 5.73, >25, >25 µM for MDA-MB-468, MDA-MB-231, HepG2, A549, U251, HCT116 cells, respectively[1].
STAT3-IN-9 (0, 0.2, 1.0, 5.0 µM; 24 h) inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701)[1].
STAT3-IN-9 (0, 0.2, 1 µM; 24 h) induces apoptosis through the mitochondrial Caspase dependent apoptotic pathway[1].
STAT3-IN-9 (0, 0.2, 1 µM; 24 h) induces cell cycle arrest at the G2/M phase in a dose-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-468, MDA-MB-231, HepG2, A549, U251, HCT116 cells
Concentration:
Incubation Time: 48 h
Result: Showed potent in vitro anti-tumor activity with IC50s of 0.16, 5.80, 1.63, 5.73, >25, >25 µM for MDA-MB-468, MDA-MB-231, HepG2, A549, U251, HCT116 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 0.2, 1.0, 5.0 µM
Incubation Time: 24 h
Result: Inhibited the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701).

Apoptosis Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 0.2, 1 µM
Incubation Time: 24 h
Result: Induced apoptosis through the mitochondrial Caspase dependent apoptotic pathway.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 0.2, 1 µM
Incubation Time: 24 h
Result: Cells were arrest at the G2/M phase in a dose-dependent manner.
Molecular Weight

391.42

Formula

C22H21N3O4

CAS No.
SMILES

COC1=CC(NC2=CC(C3=CC=NN3C)=CC4=C2OC(C(C)=O)=C4)=CC(OC)=C1

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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
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Product Name:
STAT3-IN-9
Cat. No.:
HY-146666
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