1. PI3K/Akt/mTOR Stem Cell/Wnt JAK/STAT Signaling
  2. mTOR STAT
  3. mTOR/STAT3-IN-1

mTOR/STAT3-IN-1 is a dual mTOR/STAT3 inhibitor. mTOR/STAT3-IN-1 exhibits potent mTOR inhibitory activity and moderate STAT3 inhibitory activity, while exerting cell type-dependent antiproliferative and senolytic activities in human cell lines. mTOR/STAT3-IN-1 can be used in the research of glioblastoma and aging-related diseases.

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mTOR/STAT3-IN-1

mTOR/STAT3-IN-1 Chemical Structure

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Description

mTOR/STAT3-IN-1 is a dual mTOR/STAT3 inhibitor. mTOR/STAT3-IN-1 exhibits potent mTOR inhibitory activity and moderate STAT3 inhibitory activity, while exerting cell type-dependent antiproliferative and senolytic activities in human cell lines. mTOR/STAT3-IN-1 can be used in the research of glioblastoma and aging-related diseases[1].

In Vitro

mTOR/STAT3-IN-1 (Compound 4j) (1-50 μM; 72 h) exerts cell type-dependent antiproliferative activity against BJ, RPE-1 hTERT and U-251 MG cells when applied at concentrations of 10 μM and 50 μM for 72 h[1].
mTOR/STAT3-IN-1 (1-50 μM; 72 h) inhibits the proliferation of BJ cells and induces vacuolization in BJ cells at concentrations of 10 μM and 50 μM after 72 h of treatment, but exhibits no cytotoxicity at concentrations up to 50 μM[1].
mTOR/STAT3-IN-1 (10-50 μM; 72 h) reduces the number of viable cells in Docetaxel (HY-B0011)-induced senescent BJ cells and γ-ray-induced senescent RPE-1 cells when applied at concentrations of 10 μM and 50 μM for 72 h[1].
mTOR/STAT3-IN-1 (50 μM; 72 h) reduces the confluence of Docetaxel-induced senescent BJ cells, but no cell death induced by it is detected via propidium iodide staining[1].
mTOR/STAT3-IN-1 (0.1-100 μM; 1-5 h) potently inhibits mTOR pathway activity in BJ cells. It completely inhibits the phosphorylation of p70 S6 kinase at concentrations ≥ 12.5 μM, with an IC50 value of 0.51 μM at 1 h and 0.87 μM at 5 h[1].
mTOR/STAT3-IN-1 (100 μM; 30 min) slightly inhibits IL-6-induced phosphorylation of STAT3 at Tyr705 in RPE-1 hTERT cells at a concentration of 100 μM[1].

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

Cell Proliferation Assay[1]

Cell Line: human normal dermal fibroblasts BJ, human telomerase-immortalized retinal pigment epithelial cells RPE-1 hTERT, human glioblastoma U-251 MG cells
Concentration: 1 μM, 10 μM, 50 μM
Incubation Time: 72 h
Result: Showed minimal antiproliferative activity across all three cell lines at 1 μM.
Suppressed cell growth in BJ and U-251 MG cells at 10 μM.
Suppressed cell growth in all three cell lines, with the strongest effect observed in BJ cells at 50 μM.

Cell Proliferation Assay[1]

Cell Line: human normal dermal fibroblasts BJ
Concentration: 1 μM, 10 μM, 50 μM
Incubation Time: 72 h
Result: Suppressed BJ cell proliferation at 10 μM and 50 μM.
Induced cell vacuolization at 10 μM and 50 μM.
Did not induce propidium iodide-positive cell death at any tested concentration up to 50 μM.

Cell Proliferation Assay[1]

Cell Line: docetaxel-induced senescent human normal dermal fibroblasts DTX BJ, gamma radiation-induced senescent human telomerase-immortalized retinal pigment epithelial cells IR RPE-1
Concentration: 10 μM, 50 μM
Incubation Time: 72 h
Result: Suppressed viable cell counts in both DTX BJ and IR RPE-1 senescent cell models at 10 μM and 50 μM.

Cell Proliferation Assay[1]

Cell Line: docetaxel-induced senescent human normal dermal fibroblasts DTX BJ
Concentration: 50 μM
Incubation Time: 72 h
Result: Decreased cell confluence at 50 μM.
Did not induce propidium iodide-positive cell death.

Western Blot Analysis[1]

Cell Line: human normal dermal fibroblasts BJ
Concentration: 0.1 μM, 0.5 μM, 1 μM, 5 μM, 12.5 μM, 100 μM
Incubation Time: 1 h, 5 h, unspecified time
Result: Completely suppressed p70 S6 kinase phosphorylation at 100 μM after 1 h and 5 h, and at 12.5 μM.
Showed concentration-dependent inhibition across 0.1-12.5 μM, with IC50 values of 0.51 μM after 1 h and 0.87 μM after 5 h.

Western Blot Analysis[1]

Cell Line: human telomerase-immortalized retinal pigment epithelial cells RPE-1 hTERT
Concentration: 100 μM
Incubation Time: 15 min (pre-incubation) prior to 15 min IL-6 stimulation
Result: Exhibited mild inhibition of IL-6-induced STAT3 Tyr705 phosphorylation at 100 μM.
Molecular Weight

293.32

Formula

C16H15N5O

SMILES

NC1=C2C(N(C(C)C)N=C2C3=CC4=C(C=CC=C4)O3)=NC=N1

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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
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Product Name:
mTOR/STAT3-IN-1
Cat. No.:
HY-183306
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