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Category: EnzymesarrowKinasesarrowIkB Kinase
Cat.No. Product Name
2559 TPCA-1
Price and Availability

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TPCA-1
Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophene carboxamide

Biological Activity:

Potent, selective inhibitor of IκB kinase-2 (IKK-2) (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF-κB nuclear localisation. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.

Technical Data:

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M.Wt: 279.29
Formula: C12H10FN3O2S
Storage: Desiccate at -20°C
Solubility: Soluble to 100 mM in DMSO and to 10 mM in Ethanol
Purity: >97%
CAS No: [507475-17-4]

Resources:

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    • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Podolin et al (2005) Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IκB kinase 2, TPCA-1 (2-[aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell proliferation. J.Pharmacol.Exp.Ther. 312 373. Birrell et al (2005) Iκ-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma. Am.J.Respir.Crit.Care Med. 172 962. Birrell et al (2006) IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic. Mol.Pharmacol. 69 1791.
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    Keywords: TPCA-1, Kinases, Potent, Selective Inhibitor Of IKK-2, Tocris Bioscience
    Literature in this Area
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    Product Feature
    NFκB Signalling
    Key IKK inhibitors available from Tocris include:
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    Selective inhibitor of IKK
    2611   IMD 0354
    Inhibitor of IKK-2
    2559   TPCA-1
    Potent, selective inhibitor of IKK-2
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