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50902
TPCA-1
Activators & Inhibitors
Chemical Modulators

TPCA-1 #50902

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TPCA-1: Image 1
Chemical structure of TPCA-1.

Product Usage Information

TPCA-1 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 1.19 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 279.3 g/mol
Purity >98%
Molecular Formula C12H10FN3O2S
CAS 507475-17-4
Solubility Soluble in DMSO at 30 mg/mL.

Background

TPCA-1 blocks NF-κB signaling and suppresses the transcription of several pro-inflammatory cytokines through inhibition of the IκB kinase subunit IKKβ (IKK2). Studies show that TPCA-1 specifically inhibits IKKβ (IC50 of 17.9 nM) and reduces inflammation and antigen-induced T cell proliferation in murine collagen-induced arthritis (1). TPCA-1 prevents recruitment of the transcription factor STAT3 to upstream kinases through interaction with the SH2 domain of STAT3. This limits the ability of cytokines and tyrosine kinases to induce STAT3 activity, which inhibits the ability of STAT3 to regulate cell growth and apoptosis. Treatment of non-small cell lung cancer (NSCLC) cells with TPCA-1 represses cell proliferation, suggesting that TPCA-1 may be effective in treating some forms of cancer (2). Studies have examined the ability of TPCA-1 to mediate the inflammatory response through control of IKKβ and STAT3 signaling in animal models of arthritis (1), chronic periodontitis (3), and nasal epithelial inflammation (4).
  1. Podolin, P.L. et al. (2005) J Pharmacol Exp Ther 312, 373-81.
  2. Nan, J. et al. (2014) Mol Cancer Ther 13, 617-29.
  3. Wang, B. et al. (2021) Mol Oral Microbiol 36, 192-201.
  4. Sachse, F. et al. (2011) Rhinology 49, 168-73.

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 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 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.
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To Purchase # 50902
Cat. # Size Qty. Price
50902S
5 mg
$ 85