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.
Compound Libraries
TPCA-1 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 279.29 |
| Formula | C12H10FN3O2S |
| Storage | Desiccate at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 507475-17-4 |
| PubChem ID | 9903786 |
| InChI Key | SAYGKHKXGCPTLX-UHFFFAOYSA-N |
| Smiles | NC(=O)NC1=C(C=C(S1)C1=CC=C(F)C=C1)C(N)=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.92 | 100 | |
| ethanol | 2.79 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 279.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.58 mL | 17.9 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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 J.Pharmacol.Exp.Ther. 312 373 PMID: 15316093
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
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
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, IkB, Kinase, NF-kB/IkB, IkB, Kinase, Tocris Bioscience
