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IKK-2 Inhibitor IV (CAS 507475-17-4)

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Alternate Names:
TPCA-1
Application:
IKK-2 Inhibitor IV is a potent inhibitor of IKKβ (IKK-2)
CAS Number:
507475-17-4
Purity:
>95%
Molecular Weight:
279.30
Molecular Formula:
C12H10FN3O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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IKK-2 inhibitor IV is a potent inhibitor of IKKbeta (IKK-2) which interferes with NF-kappaB DNA binding and therefore expression of many inflammatory genes. It inhibits lipopolysaccharide-induced human monocyte production of TNF-alpha and decreases the severity of murine collagen-induced arthritis. IKK-2 Inhibitor IV may act to reduce Endothelin-1 stimulated Monocyte Chemotactic Protein-1 production in human airway smooth muscle cells. It also inhibits up-regulation of bradykinin B1 and B2 receptor-mediated contractions. IKK-2 Inhibitor IV is an inhibitor of IKKalpha.


IKK-2 Inhibitor IV (CAS 507475-17-4) References

  1. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation.  |  Podolin, PL., et al. 2005. J Pharmacol Exp Ther. 312: 373-81. PMID: 15316093
  2. Ikappa-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma.  |  Birrell, MA., et al. 2005. Am J Respir Crit Care Med. 172: 962-71. PMID: 16002568
  3. IkappaB kinase-2-independent and -dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic.  |  Birrell, MA., et al. 2006. Mol Pharmacol. 69: 1791-800. PMID: 16517756
  4. Inhibition of Abeta production by NF-kappaB inhibitors.  |  Paris, D., et al. 2007. Neurosci Lett. 415: 11-6. PMID: 17223266
  5. IL-4-stimulated NF-kappaB activity is required for Stat6 DNA binding.  |  Thieu, VT., et al. 2007. J Leukoc Biol. 82: 370-9. PMID: 17513694
  6. Inhibition by a selective IkappaB kinase-2 inhibitor of interleukin-1-induced collagen degradation by corneal fibroblasts in three-dimensional culture.  |  Kondo, Y., et al. 2008. Invest Ophthalmol Vis Sci. 49: 4850-7. PMID: 18676628
  7. Transcriptional regulation of monocyte chemotactic protein-1 release by endothelin-1 in human airway smooth muscle cells involves NF-kappaB and AP-1.  |  Sutcliffe, AM., et al. 2009. Br J Pharmacol. 157: 436-50. PMID: 19371341
  8. Up-regulation of bradykinin receptors in rat bronchi via I kappa B kinase-mediated inflammatory signaling pathway.  |  Lei, Y., et al. 2010. Eur J Pharmacol. 634: 149-61. PMID: 20184874
  9. Autocrine TNF-α-mediated NF-κB activation is a determinant for evasion of CD40-induced cytotoxicity in cancer cells.  |  Li, D., et al. 2013. Biochem Biophys Res Commun. 436: 467-72. PMID: 23751348
  10. Anti-melanoma activity of Cynanchi atrati Radix is mediated by regulation of NF-kappa B activity and pro-apoptotic proteins.  |  Son, SW., et al. 2014. J Ethnopharmacol. 153: 250-7. PMID: 24583240
  11. Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1.  |  Cataldi, M., et al. 2015. Virology. 485: 340-54. PMID: 26331681
  12. Cytokine induced 3-D organotypic psoriasis skin model demonstrates distinct roles for NF-κB and JAK pathways in disease pathophysiology.  |  Todorović, V., et al. 2022. Exp Dermatol. 31: 1036-1047. PMID: 35213752
  13. A Role for p65 Signaling in Muscle-derived Stem Cell Survival and Differentiation  |  Proto, J., Lu, A., Robbins, P., & Huard, J. 2010. The FASEB Journal. 24: lb406-lb406.

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

IKK-2 Inhibitor IV, 500 µg

sc-203083
500 µg
$133.00

Does the production inhibit IKK-2 phosphorylation?

Asked by: jintt
Thank you for your question. It would be helpful if you could call 800-457-3801, allowing for a more interactive discussion of this and other related questions.
Answered by: Technical Service
Date published: 2022-03-18

Is IKK-2 inhibitor IV a reversible inhibitor?

Asked by: ChemSynth123
Thank you for your question. We do not have a reference that cites, IKK-2 Inhibitor IV, sc-203083, as a reversible inhibitor. However, sc-221743, IKK-2 Inhibitor VI, may be a reversible inhibitor of IKK-2.
Answered by: TechService7
Date published: 2017-01-27
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Rated 5 out of 5 by from CataldiCataldi, M. et al. (PubMed 26331681) demonstrated that TPCA-1 (IKK-2 Inhibitor IV) is a unique duel inhibitor of IKK- and JAK1 kinase, and provided evidence that upregulated type I interferon signaling plays a major role in resistance of pancreatic cancer cells to oncolytic viruses. -SCBT Publication Review
Date published: 2015-06-29
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IKK-2 Inhibitor IV is rated 5.0 out of 5 by 1.
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