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28992
ITD-1
Activators & Inhibitors
Chemical Modulators

ITD-1 #28992

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ITD-1: Image 1

Western blot analysis of extracts from HaCaT cells, untreated (-) or treated with hTGF-β3 #8425 and hTGF-β1 #8915 (100 ng/ml, 30 min; +) in the absence or presence of the TGFR inhibitor ITD-1 (5 μM, 18 hr; +), using Phospho-Smad2 (Ser465/467)/Smad3 (Ser423/425) (D27F4) Rabbit mAb #8828 (upper) or Smad2/3 (D7G7) XP® Rabbit mAb #8685 (lower).

ITD-1: Image 2

Chemical structure of ITD-1.

Product Usage Information

ITD-1 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.2 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 415.5 g/mol
Purity

>98%

Molecular Formula

C27H29NO3

CAS 1099644-42-4
Solubility Soluble in DMSO at 8 mg/ml or ethanol at 4 mg/ml with slight warming.

Background

ITD-1 is a potent and selective inhibitor of Transforming Growth Factor-β (TGF-β) signaling. This small molecule targets TGF-β receptor II by increasing proteasomal degradation, eliminating the receptor from the cell surface, inhibiting downstream intracellular signaling with an IC50 of 0.85 μM (1). Activation of the TGF-β receptor II leads to phosphorylation of Smad2/3 proteins, transmitting TGF-β signals from the cell surface into the nucleus. ITD-1 inhibits the phosphorylation of Smad2/3 proteins but does not block kinase activity of TGF-β receptors (type I and type II), demonstrating that ITD-1 disrupts TGF-β signaling more selectively than other kinase inhibitors (2).

  1. Schade, D. et al. (2012) J Med Chem 55, 9946-57.
  2. Willems, E. et al. (2012) Cell Stem Cell 11, 242-52.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.
To Purchase # 28992S
Product # Size Price
28992S
5 mg $ 105