Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Biological ActivityPotent, 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
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.
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
A CD47-associated super-enhancer links pro-inflammatory signalling to CD47 upregulation in breast cancer.
Nat Commun 2017;8:14802
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
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
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.
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
IKK2 inhibition attenuates laser-induced choroidal neovascularization.
Authors: Lu Et al.
Open Biol 2014;9:e87530
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
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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