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Description: Potent, selective inhibitor of IKKβ
Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Purity: ≥97% (HPLC)
Biological Activity for TPCA-1
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.
Compound Libraries for TPCA-1
TPCA-1 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for TPCA-1
| M. Wt | 279.29 |
| Formula | C12H10FN3O2S |
| Storage | Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TPCA-1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.92 | 100 |
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 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 |
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Product Datasheets for TPCA-1
References for TPCA-1
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TPCA-1, please let us know.
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Keywords: TPCA-1, 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, 2559, Tocris Bioscience
8 Citations for TPCA-1
Citations are publications that use Tocris products. Selected citations for TPCA-1 include:
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
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
Betancur (2017) A CD47-associated super-enhancer links pro-inflammatory signalling to CD47 upregulation in breast cancer. Nat Commun 8 14802 PMID: 28378740
Cataldi et al (2015) Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1. Virology 485 340 PMID: 26331681
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
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
Do you know of a great paper that uses TPCA-1 from Tocris? Please let us know.
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