ITD-1
Based on 6 publication(s) in Google Scholar
ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.77%
- No. CAS: 1099644-42-4
- Fòrmula: C27H29NO3
- Peso molecular:415.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ITD-1
More- Int J Biol Sci. 2025 Sep 12;21(13):5821-5841. [Abstract]
- Sci China Life Sci. 2025 Mar;68(3):746-763. [Abstract]
- Cell Rep. 2022 Jun 21;39(12):110986. [Abstract]
- Cancer Manag Res. 2022 Jan 26;14:327-337. [Abstract]
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- Oncotarget. 2017 Dec 14;9(3):3188-3197. [Abstract]
Customer Validation & Images
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WB
Actividad biológica
Descripciòn
IC50 & Target
IC50: 460 nM (TGFβ receptor)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.85 μM
Compound: 1
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Inhibition of TGFbeta/Smad in TGFbeta-2/activin A-stimulated HEK293 cells preincubated for 2 hrs before stimulation measured after 20 to 22 hrs by firefly/renilla luciferase reporter assay
Inhibition of TGFbeta/Smad in TGFbeta-2/activin A-stimulated HEK293 cells preincubated for 2 hrs before stimulation measured after 20 to 22 hrs by firefly/renilla luciferase reporter assay
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[PMID: 25817775] |
In Vitro
ITD-1 potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A. HEK293T cells are transfected with a Smad4 response element driving luciferase (SBE4-Luc) to test whether ITD-1 blocks Activin A/Nodal and/or TGFβ signaling, which utilize the same intracellular signaling cascade through Smad4. ITD-1 strongly inhibits TGFβ2 signaling with similar efficacy (92% vs. 99% respectively), but with lower potency compared to SB-431542, an ACVR1B/TGFBR1 kinase inhibitor (IC50= 850nM vs. 70nM respectively), and is a weak and partial inhibitor of Activin A signals. ITD-1 selectively enhances the differentiation of uncommitted mesoderm to cardiomyocytes, but not to vascular smooth muscle and endothelial cells. ITD-1 reveals an unexpected role for TGFβ signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1099644-42-4
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Appearance Solid
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Peso molecular 415.52
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Fòrmula C27H29NO3
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Color Light yellow to yellow
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SMILES
O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C(C4=CC=CC=C4)C=C3)OCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
2025 Sep 12;21(13):5821-5841. PMID: 41079923 -
Sci China Life Sci
Integrating spatial transcriptomics and single-nucleus RNA-seq revealed the specific inhibitory effects of TGF-β on intramuscular fat deposition. [Abstract]2025 Mar;68(3):746-763. PMID: 39422812 -
Cell Rep
Tumor metabolite lactate promotes tumorigenesis by modulating MOESIN lactylation and enhancing TGF-β signaling in regulatory T cells. [Abstract]2022 Jun 21;39(12):110986. PMID: 35732125 -
Cancer Manag Res
Exosomal lncRNA ATB Derived from Ovarian Cancer Cells Promotes Angiogenesis via Regulating miR-204-3p/TGFβR2 Axis. [Abstract]2022 Jan 26;14:327-337. PMID: 35115831 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
Oncotarget
Hypoxia-inducible factor-1α activates transforming growth factor-β1/Smad signaling and increases collagen deposition in dermal fibroblasts. [Abstract]2017 Dec 14;9(3):3188-3197. PMID: 29423039
ITD-1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Dec 14;9(3):3188-3197. [Abstract]
Treatment with 5 μM ITD-1, DMSO, and blank, respectively, for 24 h under 1% O2 condition. ITD-1 inhibits the phosphorylation of Smad2/3 by inhibiting TβRII. Meanwhile, HIF-1α and Smad2/3 levels remain stable in all three groups. The histogram shows the protein band intensity ratio of p-Smad2 to Smad2 and p-Smad3 to Smad3.
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (240.66 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
Cell Assay
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Willems E, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells. Cell Stem Cell. 2012 Aug 3;11(2):242-52. [Content Brief]
[2]. Schade D, Lanier M, Willems E, et al. Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling. J Med Chem. 2012;55(22):9946-9957. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4066 mL | 12.0331 mL | 24.0662 mL | 60.1656 mL |
| 5 mM | 0.4813 mL | 2.4066 mL | 4.8132 mL | 12.0331 mL | |
| 10 mM | 0.2407 mL | 1.2033 mL | 2.4066 mL | 6.0166 mL | |
| 15 mM | 0.1604 mL | 0.8022 mL | 1.6044 mL | 4.0110 mL | |
| 20 mM | 0.1203 mL | 0.6017 mL | 1.2033 mL | 3.0083 mL | |
| 25 mM | 0.0963 mL | 0.4813 mL | 0.9626 mL | 2.4066 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8022 mL | 2.0055 mL | |
| 40 mM | 0.0602 mL | 0.3008 mL | 0.6017 mL | 1.5041 mL | |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4813 mL | 1.2033 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL | |
| 100 mM | 0.0241 mL | 0.1203 mL | 0.2407 mL | 0.6017 mL |
ITD-1 Related Classifications
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