TPCA-1

Key Product Details

Product Description

TPCA-1 is a 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.

Product Specifications for TPCA-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for TPCA-1

The following data is based on the product molecular weight 279.29.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

6 5 4 3 2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.58 mL	17.90 mL	35.81 mL
5 mM	0.72 mL	3.58 mL	7.16 mL
10 mM	0.36 mL	1.79 mL	3.58 mL
50 mM	0.07 mL	0.36 mL	0.72 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 73 publications citing the usage of this product.

• Birrell IK-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma. Am.J.Respir.Crit.Care Med. 2005 PMID: 16002568
• Birrell IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic. Mol.Pharmacol. 2006 PMID: 16517756
• Podolin 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 J.Pharmacol.Exp.Ther. 2005 PMID: 15316093

Product Documents for TPCA-1