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TPCA-1

Cat. No. 2559 8 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 Technical Data Solubility Calculators Datasheets References

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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Safety Datasheet

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:

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

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

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

Do you know of a great paper that uses TPCA-1 from Tocris? Please let us know.

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