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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

TGF-β1/Smad3-IN-1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

TGF-β1/Smad3-IN-1 Related Antibodies

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
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (172.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7281 mL 8.6404 mL 17.2807 mL
5 mM 0.3456 mL 1.7281 mL 3.4561 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (8.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (8.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7281 mL 8.6404 mL 17.2807 mL 43.2018 mL
5 mM 0.3456 mL 1.7281 mL 3.4561 mL 8.6404 mL
10 mM 0.1728 mL 0.8640 mL 1.7281 mL 4.3202 mL
15 mM 0.1152 mL 0.5760 mL 1.1520 mL 2.8801 mL
20 mM 0.0864 mL 0.4320 mL 0.8640 mL 2.1601 mL
25 mM 0.0691 mL 0.3456 mL 0.6912 mL 1.7281 mL
30 mM 0.0576 mL 0.2880 mL 0.5760 mL 1.4401 mL
40 mM 0.0432 mL 0.2160 mL 0.4320 mL 1.0800 mL
50 mM 0.0346 mL 0.1728 mL 0.3456 mL 0.8640 mL
60 mM 0.0288 mL 0.1440 mL 0.2880 mL 0.7200 mL
80 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5400 mL
100 mM 0.0173 mL 0.0864 mL 0.1728 mL 0.4320 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

TGF-β1/Smad3-IN-1 Related Classifications

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-1TGF-beta/SmadTransforming growth factor betaAnti fibroticOral activitySD ratsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TGF-β1/Smad3-IN-1
Cat. No.:
HY-163536
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.