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54678
LY-364947
Activators & Inhibitors
Chemical Modulators

LY-364947 #54678

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Citations (0)
LY-364947: Image 1

Western blot analysis of extracts from HT-1080 cells, untreated (-) or treated with Human Transforming Growth Factor β1 (hTGF-β1) #8915 (10 ng/ml, 30 min; +) with or without pretreating the cells with LY-364947 (1 μM, 1 hr; +), using Phospho-Smad2 (Ser465/467)/Smad3 (Ser423/425) (D27F4) Rabbit mAb #8828 (upper), Smad2/3 (D7G7) XP® Rabbit mAb #8685 (middle), and β-Actin (D6A8) Rabbit mAb #8457 (lower).

LY-364947: Image 2

Chemical structure of LY-364947.

Product Usage Information

LY-364947 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 1.22 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at room temperature, 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 272.3 g/mol
Purity

>98%

Molecular Formula

C17H12N4

CAS 396129-53-6
Solubility Soluble in DMSO at 25 mg/ml.

Background

LY-364947, also known as HTS-466284, is a potent and selective TGF-β type-I receptor (TGF-β RI, TGFR-I, TβR-I, ALK-5) inhibitor. This small molecule specifically targets TGF-β RI with an IC50 value of 59 nM and is less effective on TGF-β RII and MLK-7K (IC50 values of 400 nM and 1400 nM, respectively) (1). LY-364947 regulates MDA-MB-231 cell invasion by inhibiting autocrine TGF-β signaling (2). Patients in intensive care units (ICUs) that suffer from chronic sepsis can experience weakening of the diaphragm muscles caused by muscle wasting, requiring mechanical ventilation. Members of the TGF-β family can trigger the activation of protein breakdown. Inhibition of the TGF-β pathway can protect the diaphragm during chronic sepsis, making LY-364947 an interesting compound to study as it relates to effective ICU patient care (3).

  1. Sawyer, J.S. et al. (2003) J Med Chem 46, 3953-6.
  2. Shiou, S.R. et al. (2006) J Biol Chem 281, 33971-81.
  3. Jude, B. et al. (2019) Shock , doi: 10.1097/SHK.0000000000001393.

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 # 54678S
Product # Size Price
54678S
5 mg $ 119