1. TGF-beta/Smad
  2. TGF-β Receptor
  3. ITD-1

ITD-1 

Cat. No.: HY-12704 Purity: 99.96%
Handling Instructions

ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.

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

ITD-1 Chemical Structure

ITD-1 Chemical Structure

CAS No. : 1099644-42-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 190 In-stock
Estimated Time of Arrival: December 31
100 mg USD 290 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ITD-1 purchased from MCE. Usage Cited in: Oncotarget. 2017 Dec 14;9(3):3188-3197.

    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.

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    • Biological Activity

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    • References

    • Customer Review

    Description

    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.

    IC50 & Target

    IC50: 460 nM (TGFβ receptor)

    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.

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

    Molecular Weight

    415.52

    Formula

    C₂₇H₂₉NO₃

    CAS No.
    SMILES

    O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C(C4=CC=CC=C4)C=C3)OCC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 28 mg/mL (67.39 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4066 mL 12.0331 mL 24.0662 mL
    5 mM 0.4813 mL 2.4066 mL 4.8132 mL
    10 mM 0.2407 mL 1.2033 mL 2.4066 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay

    For the Smad4-Response element (SBE4) assay, 293T cells are grown in Phenol Free DMEM-high glucose supplemented with 1% FBS. About 30000 cells/cm2 are reverse transfected onto white 384-well cell-culture plates with 10ng of SBE4-Lux and CMV-Renilla-Lux using Lipofectamine 2000. Cells are allowed to adhere for at least 12 hours and induced with either TGFβ2 (15 ng/mL), Activin A (15 ng/mL). Simultaneously, ITD-1 (0.001, 0.01, 0.1, 1, and 10 μM) is added to cells. SB-431542 is used as a positive control for Activin A/TGFβ-signaling inhibition. To determine luminescence levels, Dual-Glo kit is used and measured on an Envision plate reader. Firefly luminescence is normalized against renilla luciferase.

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

    References

    Purity: 99.96%

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    Keywords:

    ITD-1ITD1ITD 1TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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    Cat. No.:
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