TPCA-1
Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Purity: ≥97%
Biological Activity
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.Technical Data
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.
Background References
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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
Podolin et al.
J.Pharmacol.Exp.Ther., 2005;312:373 -
IK-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma.
Birrell et al.
Am.J.Respir.Crit.Care Med., 2005;172:962 -
IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic.
Birrell et al.
Mol.Pharmacol., 2006;69:1791
Product Datasheets
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Citations for TPCA-1
The citations listed below are publications that use Tocris products. Selected citations for TPCA-1 include:
8 Citations: Showing 1 - 8
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A CD47-associated super-enhancer links pro-inflammatory signalling to CD47 upregulation in breast cancer.
Authors: Betancur
Nat Commun 2017;8:14802
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NEMO regulates a cell death switch in TNF signaling by inhibiting recruitment of RIPK3 to the cell death-inducing complex II.
Authors: Pescatore Et al.
Cell Death & Disease 2016;7:e2346
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Fractalkine shedding is mediated by p38 and the ADAM10 protease under pro-inflammatory conditions inhuman astrocytes.
Authors: O'Sullivan Et al.
Journal of Neuroinflammation 2016;13:189
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Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1.
Authors: Cataldi Et al.
Virology 2015;485:340
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IKK2 Inhibition Using TPCA-1-Loaded PLGA Microparticles Attenuates Laser-Induced Choroidal Neovascularization and Macrophage Recruitment.
Authors: Gaddipati Et al.
PLoS One 2015;10:e0121185
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IKK2 inhibition attenuates laser-induced choroidal neovascularization.
Authors: Lu Et al.
Open Biol 2014;9:e87530
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Regulation of large conductance Ca2+-activated K+ (BK) channel β1 subunit expression by muscle RING finger protein 1 in diabetic vessels.
Authors: Yi Et al.
J Biol Chem 2014;289:10853
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TNFR1 and TNFR2 regulate the extrinsic apoptotic pathway in myeloma cells by multiple mechanisms.
Authors: Rauert Et al.
Cell Death Dis 2011;2:e194
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