TPCA-1

Name: TPCA-1
Brand: Tocris Bioscience
SKU: 2559
Price: 301 USD

Tocris Bioscience a Bio-Techne Brand

Catalog # 2559

Citations (8)

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Key Product Details

Description:	Potent, selective inhibitor of IKKβ
Chemical Name:	2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Purity:	≥97% (HPLC)
Molecular Weight:	279.29

View Full Technical Details for TPCA-1

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 for TPCA-1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	17.90 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

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References for TPCA-1

References are publications that support the biological activity of the product.

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
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

Citations for TPCA-1 (8)

Showing 1 - 8 of 8 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for TPCA-1 include:

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

There are no citations that match your criteria.