1. TGF-beta/Smad
  2. TGF-β Receptor
  3. TGFβ1-IN-5

TGFβ1-IN-5 is a TGF-β1 inhibitor with blood-brain barrier permeability. TGFβ1-IN-5 reduces extracellular TGF-β1 levels in glioblastoma cells. TGFβ1-IN-5 exerts antiproliferative, antimigratory and clonogenic inhibitory effects in glioblastoma cells while maintaining the viability of non-cancerous cells. TGFβ1-IN-5 can be used for the research of glioblastoma.

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

TGFβ1-IN-5

TGFβ1-IN-5 Chemical Structure

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Description

TGFβ1-IN-5 is a TGF-β1 inhibitor with blood-brain barrier permeability. TGFβ1-IN-5 reduces extracellular TGF-β1 levels in glioblastoma cells. TGFβ1-IN-5 exerts antiproliferative, antimigratory and clonogenic inhibitory effects in glioblastoma cells while maintaining the viability of non-cancerous cells. TGFβ1-IN-5 can be used for the research of glioblastoma[1].

In Vitro

TGFβ1-IN-5 (Compound 3e) (0-100 μM; 24 h) exhibits moderately potent selective antiproliferative activity against U87 cells (IC50 = 41.09 μM), while showing no significant inhibitory effect on non-cancerous cells BEAS-2B and HUVEC[1].
TGFβ1-IN-5 (41 μM; 24 h) reduces extracellular TGF-β1 levels in U87 glioblastoma cells[1].
TGFβ1-IN-5 (20-80 μM; 24 h) reduces the number of U87 glioblastoma cells in a concentration-dependent manner, but exerts no significant effect on the number of non-cancerous HUVEC cells[1].
TGFβ1-IN-5 (41 μM; 72 h) significantly inhibits the migration of U87 glioblastoma cells in a time-dependent manner[1].
TGFβ1-IN-5 (41 μM; 5 days) inhibits the long-term clonogenic potential of U87 glioblastoma cells[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: U87 cells, BEAS-2B cells, HUVEC cells
Concentration: 0,
1.5, 3.1, 6.2, 12.5, 25, 50, and 100 μM
Incubation Time: 24 h
Result: Showed moderate anti-proliferative activity in U87 cells with an IC50 of 41.09 μM.
Maintained high viability in non-cancerous cells, with IC50 values ≥96.60 μM in BEAS-2B and HUVEC cells.
Increased cell number in HUVEC and BEAS-2B cells at concentrations ≤3.125 μM.
Increased cell number in U87 cells at concentrations ≤12.5 μM.

ELISA Assay[1]

Cell Line: human glioblastoma U87 cells
Concentration: 41 μM
Incubation Time: 24 h
Result: Caused a 5.5% decrease in extracellular TGF-β1 levels (88.90 pg/mL) compared to untreated control cells (94.11 pg/mL).

Cell Migration Assay [1]

Cell Line: human glioblastoma U87 cells
Concentration: 41 μM
Incubation Time: 72 h
Result: Significantly delayed wound closure compared to control cells at all time points.
Molecular Weight

553.45

Formula

C31H25BrN2O3

SMILES

O=C(C1=CC=CC=C1)/C=C/C2=CC=C(N3C=[N+](CC4=CC=C(C(OC)=O)C=C4)C5=CC=CC=C35)C=C2.[Br-]

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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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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.

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Product Name:
TGFβ1-IN-5
Cat. No.:
HY-183258
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