ITD-1

Name: ITD-1
Brand: MedChemExpress
SKU: HY-12704
Rating: 5.0 (6 reviews)

Cat. No.: HY-12704 Purity: 99.41%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1099644-42-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 209	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 319	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

5 Publications Citing Use of MCE ITD-1

: 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.

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

Biological Activity
Protocol
Purity & Documentation
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)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.85 μM Compound: 1	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	[PMID: 25817775]
HEK-293T	IC₅₀	0.46 μM Compound: (+)1	Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay	[PMID: 23130626]
HEK-293T	IC₅₀	0.85 μM Compound: 1	Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay	[PMID: 23130626]
HEK-293T	IC₅₀	6.9 μM Compound: (-)1	Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay	[PMID: 23130626]

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.

Molecular Weight

415.52

Formula

C₂₇H₂₉NO₃

CAS No.

1099644-42-4

Appearance

Solid

Color

Light yellow to yellow

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 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

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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

Purity: 99.41%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (252 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

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

[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]

Complete Stock Solution Preparation Table

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

ITD-1 Related Classifications

Cardiovascular Disease

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:

ITD-11099644-42-4ITD1ITD 1TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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ITD-1

Customer Review

ITD-1 Related Antibodies

5 Publications Citing Use of MCE ITD-1

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•Related Screening Libraries:

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View All TGF-β Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

ITD-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ITD-1 Related Classifications

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