TGF-β2-IN-1
TGF-β2-IN-1 is a selective TGF-β2 inhibitor. TGF-β2-IN-1 exhibits potent antiproliferative effects on HCT-116, Caco-2 and HT-29 with IC50 values of 6.84, 10.21, and 9.47 μM, respectively. TGF-β2-IN-1 inhibits TGF-β2 signaling in a dose-dependent manner by suppressing both receptor and cytokine expression.TGF-β2-IN-1 can be used for the study of colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C25H22ClN5O3
- Molecular Weight:475.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
TGF-β2-IN-1 (Compound 10k) (1.562-100 μM, 48 h) exhibits potent antiproliferative effects on HCT-116 (IC50 = 6.84 μM), Caco-2 (IC50 = 10.21 μM) and HT-29 (IC50 = 9.47 μM)[1]. TGF-β2-IN-1 (1.562-100 μM, 48 h) leads to progressive reductions in TGF-β2 receptor levels and TGF-β2 cytokine levels in HCT-116 cells[1]. TGF-β2-IN-1 (50-100 μM, 48 h) does not significantly induce apoptosis or necrosis in HCT-116 cells[1]. TGF-β2-IN-1 exhibits strong binding affinity towards the TGF-β receptor type II with an IFD XP Glide score of 11.28 kcal/mol[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:1.562, 3.125, 6.25, 12.5, 25, 50, 100 μM
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Incubation Time:48 h
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Result:Led to progressive reductions in TGF-β2 receptor levels and TGF-β2 cytokine levels in HCT-116 cells.
Showed more pronounced inhibition of the receptor component of the pathway than Sorafenib (HY-10201).
Chemical Information
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Molecular Weight 475.93
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Formula C25H22ClN5O3
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SMILES
COC1=CC=CC(/C=N/NC(C2=CC=CC=C2OCC3=CN(N=N3)CC4=CC(Cl)=CC=C4)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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