2. Vitamin D Related/Nuclear Receptor TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. VD/VDR TGF-beta/Smad Collagen Hippo (MST)
  4. TGF-β1/Smad3-IN-2

TGF-β1/Smad3-IN-2 is an orally active antifibrotic agent. TGF-β1/Smad3-IN-2 has high affinity for VDR and can inhibit the TGFβ/SMAD3 signaling pathway. TGF-β1/Smad3-IN-2 inhibits hepatic stellate cell activation, reduces extracellular matrix deposition, and alleviates liver fibrosis in a bile duct ligation mouse model. TGF-β1/Smad3-IN-2 can be used for the research of liver fibrosis.

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

TGF-β1/Smad3-IN-2

TGF-β1/Smad3-IN-2 Chemical Structure

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TGF-β1/Smad3-IN-2 Related Antibodies

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Description

TGF-β1/Smad3-IN-2 is an orally active antifibrotic agent. TGF-β1/Smad3-IN-2 has high affinity for VDR and can inhibit the TGFβ/SMAD3 signaling pathway. TGF-β1/Smad3-IN-2 inhibits hepatic stellate cell activation, reduces extracellular matrix deposition, and alleviates liver fibrosis in a bile duct ligation mouse model. TGF-β1/Smad3-IN-2 can be used for the research of liver fibrosis[1].

In Vitro

TGF-β1/Smad3-IN-2 (compound D13) (0.1 μM; 24 h) significantly downregulates the Collagen I (COL1A1) and α-SMA (ACTA2) markers in TGF-β1-induced human LX-2 hepatic stellate cells (HSCs)[1].
TGF-β1/Smad3-IN-2 exhibits extremely low cytotoxicity in human hepatic stellate cell line LX-2, with an IC50 > 50 μM[1].
TGF-β1/Smad3-IN-2 (0.1 μM; 48 h) induces 654 downregulated differentially expressed genes and 507 upregulated DEGs in TGF-β1-stimulated human hepatic stellate cell line LX-2, among which core fibrotic genes (COL1A1, COL1A2, COL3A1) are significantly downregulated, with significant enrichment in the TGF-β signaling pathway, ECM-receptor interaction pathway and Hippo signaling pathway[1].
TGF-β1/Smad3-IN-2 promotes the direct interaction between VDR and SMAD3 proteins in human hepatic stellate cell line LX-2[1].

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

TGF-β1/Smad3-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: LX-2 human hepatic stellate cells (HSCs)
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Reduced α-SMA and collagen I protein levels to near baseline.
In Vivo

TGF-β1/Smad3-IN-2 (100 μg/kg; oral gavage; once daily; for 2 consecutive weeks) exhibits antifibrotic efficacy in a mouse model of bile duct ligation-induced hepatic fibrosis[1].

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

Animal Model: C57BL/6 (male, 8 weeks old, liver fibrosis induced by common bile duct ligation)[1]
Dosage: 100 μg/kg
Administration: oral gavage; once daily; 2 weeks
Result: Markedly ameliorated hepatic inflammation and reduced collagen accumulation in liver tissue, with efficacy comparable to calcipotriol.
Significantly downregulated hepatic expression of pro-fibrotic genes Ctgf, Fn, and Timp-1.
Significantly reduced serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bile acids (TBA).
Did not induce significant changes in serum calcium levels.
Molecular Weight

565.78

Formula

C38H47NO3
SMILES

O=C(N(CC1=CC=CC=C1)CC2=CC=CC=C2)/C=C/[C@H]([C@H]3CC[C@H]([C@]3(C)CCC/4)C4=C\C=C(C[C@@H](O)C[C@@H]5O)/C5=C)C
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-β1/Smad3-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-β1/Smad3-IN-2VD/VDRTGF-beta/SmadCollagenHippo (MST)Vitamin DVitamin D receptorTransforming growth factor betabile duct ligation mouse modelHEK293 cellsVDRliver fibrosisextracellular matrixhepatic stellate cellTGFβ/SMAD3 signalingCaco-2 intestinal cellsSMAD3LX-2 human HSCsInhibitorinhibitorinhibit

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