TPCA-1

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Description: Potent, selective inhibitor of IKKβ
Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Purity: ≥97% (HPLC)
Datasheet
Citations (8)
Reviews

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.

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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Product Action

View all IκB Kinase Inhibitors

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

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

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

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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