TPCA-1

Name: TPCA-1
Brand: Tocris Bioscience
SKU: 2559

Tocris Bioscience, part of Bio-Techne | Catalog # 2559

Citations (89)

COA / SDS

Potent, selective inhibitor of IKKβ

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

Technical Data
Citations

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 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
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