1. Stem Cell/Wnt TGF-beta/Smad
  2. TGF-beta/Smad
  3. TGF-β1/Smad3-IN-1

TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency.

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

TGF-β1/Smad3-IN-1 Chemical Structure

TGF-β1/Smad3-IN-1 Chemical Structure

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Description

TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency[1].

In Vitro

TGF-β1/Smad3-IN-1 (100-500 nM; 48 h) leads to a decrease in TGF-β1 levels in H2228 cells, which is better inhibited than Nintedanib (HY-50904) at the same concentration[1].
TGF-β1/Smad3-IN-1 (2-6 μM; 24 h) shows dose-dependent inhibition of p-Smad3 and α-SMA expression and significantly inhibits NIH3T3 cell migration[1].
TGF-β1/Smad3-IN-1 (3-10 μM; 72 h) increases Cleave-casepase3 expression in NIH3T3 cells and dose-dependently induces apoptosis[1].
TGF-β1/Smad3-IN-1 has an IC50 of 1.07 μM for NIH3T3 cells. IC50 for TGFβ1-activated HFL1 cells is 2.86 μM. TGF-β1/Smad3-IN-1 is found to be effective in inhibiting the expression of α-SMA[1].

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

Apoptosis Analysis[1]

Cell Line: NIH3T3
Concentration: 3, 7.5, 10 μM
Incubation Time: 72 h
Result: At the highest concentration of 10 μM, the total apoptosis rate of cells reached 91.79%, indicating that 5aa has a strong ability to induce apoptosis.
In Vivo

TGF-β1/Smad3-IN-1 is more bioavailable than Nintedanib in SD rats[1].
TGF-β1/Smad3-IN-1 (p.o.; 100 mg/kg/; day 2-20) inhibits bleomycin-induced pulmonary TGFβ1 and HYP expression, reduces extracellular mesenchymal deposition, and attenuates pulmonary fibrosis in bleomycin-induced model of pulmonary fibrosis in mice[1].


Pharmacokinetic Analysis in SD rats[1]

Route Dose (mg/kg) Tmax (h) t1/2 (h) Vz_F_obs (L/kg) MRT0~t (h) AUC0~t-Dobs (h·ng/mL/mg) F (%)
p.o. 10 3.01 ± 1.24 3.85 ± 0.31 / 5.117 ± 1.23 203.540 ± 4.7 15.96 ± 4.67
i.v. 1 0.029 ± 0.001 2.577 ± 0.33 19.636 ± 1.48 / 127.471 ± 25.41 /


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

Animal Model: Bleomycin-induced model of pulmonary fibrosis in mice[1]
Dosage: 100 mg/kg/
Administration: p.o.; day 2-20
Result: Significantly reduced α-SMA, fibronection and p-smad3 protein expression levels.
Significantly reduced TGFβ1 levels, more effective than Nintedanib.
Reduced hydroxyproline (HYP) levels.
Molecular Weight

578.68

Formula

C30H34N4O6S

SMILES

O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N4CCN(C)CC4)C=C3)/C5=CC=CC=C5)OC.CCS(=O)(O)=O

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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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TGF-β1/Smad3-IN-1 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.

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Product Name:
TGF-β1/Smad3-IN-1
Cat. No.:
HY-163536
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