2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. TGF-β/Smad-IN-2

TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. TGF-β/Smad-IN-2 inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation and collagen deposition, with an IC50 value of 102 μM for collagen reduction in LL29 cells. TGF-β/Smad-IN-2 exerts its effects through modulation of the SMAD3/SMAD7 signaling pathway. TGF-β/Smad-IN-2 reduces lung index in pulmonary fibrosis mice. TGF-β/Smad-IN-2 can be used for the study of pulmonary fibrosis.

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TGF-β/Smad-IN-2

TGF-β/Smad-IN-2 Chemical Structure

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TGF-β/Smad-IN-2 Related Antibodies

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Description

TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. TGF-β/Smad-IN-2 inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation and collagen deposition, with an IC50 value of 102 μM for collagen reduction in LL29 cells. TGF-β/Smad-IN-2 exerts its effects through modulation of the SMAD3/SMAD7 signaling pathway. TGF-β/Smad-IN-2 reduces lung index in pulmonary fibrosis mice. TGF-β/Smad-IN-2 can be used for the study of pulmonary fibrosis[1].

In Vitro

TGF-β/Smad-IN-2 (Compound 10b) (50-100 μM, 48 h) significantly downregulates mRNA expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, COLLAGEN3α1, TIMP1, VIMENTIN) and inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation in LL29 cells and DHLF cells[1].
TGF-β/Smad-IN-2 (50-100 μM, 48 h) reduces protein levels of α-SMA, COLLAGEN3α1, and p-COFILIN in DHLF cells and restores E-CADHERIN expression under TGF-β stimulation[1].

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

TGF-β/Smad-IN-2 Related Antibodies

Real Time qPCR[1]

Cell Line: LL29 cells and DHLF cells
Concentration: 50,100 μM
Incubation Time: 48 h
Result: Downregulated mRNA expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, COLLAGEN3α1, TIMP1, VIMENTIN).
In Vivo

TGF-β/Smad-IN-2 (Compound 10b) (150-300 mg/kg, i.g., once daily, 14 days) improves body weight recovery and survival rate, and reduces lung index in Bleomycin (BLMN) (HY-17565A)-induced pulmonary fibrosis C57BL/6 mice[1].

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

Animal Model: BLMN (2 mg/kg in normal saline) was intratracheally administered to 6-week-old male C57BL/6 mice to establish the pulmonary fibrosis model[1]
Dosage: 150, 300 mg/kg
Administration: i.g., once daily, 14 days
Result: Achieved lung index reduction.
Showed no significant changes in body weight and no abnormal hematological parameters (RBC, WBC, hemoglobin, platelets) or pathological changes.
Reduced the mRNA and protein expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, TIMP3) in lung tissues.
Appeared downregulation of phosphorylated Smad3 and upregulation of Smad7 in lung tissues.
Showed improvement in lung function (reduced respiratory resistance and elastance, increased quasi-static compliance).
Achieved reduction in collagen deposition in lung tissues.
Molecular Weight

284.35

Formula

C17H20N2O2
SMILES

O=C1C(CN2CCOCC2)=CC(C)=CN1C3=CC=CC=C3
Shipping

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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TGF-β/Smad-IN-2 Related Classifications

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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.

Keywords:

TGF-β/Smad-IN-2TGF-beta/SmadTransforming growth factor betapulmonary fibrosisTGF-β/SmadLL29 cellsDHLF cellsInhibitorinhibitorinhibit

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