TPCA-1

Cat. No. 2559

TPCA-1 C12H10FN3O2S [507475-17-4]

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Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide

Biological Activity

Potent, selective inhibitor of IκB kinase (IKK) β (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKKα 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 localization. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.

Technical Data

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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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. PMID: 16517756.

Birrell et al (2005) IK-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. PMID: 16002568.

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. PMID: 15316093.

If you know of a relevant reference for TPCA-1 please let us know.

Citations are publications that use Tocris products. Selected citations for TPCA-1 include:

Betancur (2017) A CD47-associated super-enhancer links pro-inflammatory signalling to CD47 upregulation in breast cancer. Nat Commun 8 14802. PMID: 28378740.

O'Sullivan et al (2016) Fractalkine shedding is mediated by p38 and the ADAM10 protease under pro-inflammatory conditions inhuman astrocytes. Journal of Neuroinflammation 13 189. PMID: 27549131.

Pescatore et al (2016) NEMO regulates a cell death switch in TNF signaling by inhibiting recruitment of RIPK3 to the cell death-inducing complex II. Cell Death & Disease 7 e2346. PMID: 27560715.

Gaddipati et al (2015) IKK2 Inhibition Using TPCA-1-Loaded PLGA Microparticles Attenuates Laser-Induced Choroidal Neovascularization and Macrophage Recruitment. PLoS One 10 e0121185. PMID: 25803615.

Lu et al (2014) IKK2 inhibition attenuates laser-induced choroidal neovascularization. Open Biol 9 e87530. PMID: 24489934.

Yi et al (2014) Regulation of large conductance Ca2+-activated K+ (BK) channel β1 subunit expression by muscle RING finger protein 1 in diabetic vessels. J Biol Chem 289 10853. PMID: 24570002.

Rauert et al (2011) TNFR1 and TNFR2 regulate the extrinsic apoptotic pathway in myeloma cells by multiple mechanisms. Cell Death Dis 2 e194. PMID: 21850048.

Do you know of a great paper that uses TPCA-1 from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: TPCA-1, supplier, Potent, selective, inhibitors, inhibits, IKK-2, IκB, IkappaB, kinases, Nuclear, Factor, Kappa, B, NF-κB, NF-kappaB, NF-kB, Cytokine, Signaling, Signalling, Transcription, Factors, Tocris Bioscience, IκB Kinase Inhibitor products

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