R&D Systems Inc. Tocris Bioscience Boston Biochem

TPCA-1

Cat. No. 2559

TPCA-1 C12H10FN3O2S [507475-17-4]

Price and Availability

For TPCA-1 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide

Biological Activity

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

M.Wt:
279.29
Formula:
C12H10FN3O2S
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>97 %
Storage:
Desiccate at -20°C
CAS No:
507475-17-4

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View Safety Data Sheet

References

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.

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 antigen-induced T cell proliferation. J.Pharmacol.Exp.Ther. 312 373. PMID: 15316093.

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 citation for this product please let us know.

Keywords: TPCA-1, supplier, Potent, selective, inhibitors, IKK-2, IκB, IkappaB, kinases, Nuclear, Factor, Kappa, B, NF-κB, NF-kappaB, NF-kB, Cytokine, Signaling, Signalling, Transcription, Factors

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Guide

Highlights over 350 products for cancer research. Request a copy or view PDF today.

divider line

Kinases Product Listing

Kinases Product Listing

Highlights over 350 products for kinase research. Request a copy or view PDF today.

divider line

Kinase Inhibitor Toolbox

80 Kinase inhibitors
pre-dissolved in DMSO

Some of the most potent
kinase inhibitors all on one plate

Includes many of the latest kinase inhibitors to become commercially available. Covers a wide range of kinase targets including EGFR, MAPK and CDK.

divider line

Immunology Guide

Immunology Research Guide

Highlights over 150 products for immunology research. Request a copy or view PDF today.

divider line

New Product Guide

NPG

Highlights 140 new products added in the first half of 2014. Request a copy or view PDF today.

divider line

New Products in this Area

KN 93 phosphate

CaM kinase II inhibitor; water soluble version of KN-93 (Cat. No. 1278).

Bryostatin 3

Potent protein kinase C activator

GKA 50

Glucokinase activator

MRT 67307 dihydrochloride

Salt inducible kinase (SIK) inhibitor

LDN 209929 dihydrochloride

Potent and selective haspin kinase inhibitor

RKI 1447 dihydrochloride

Potent and selective ROCK inhibitor; antitumor

LIMKi 3

Potent LIM kinase inhibitor; antitumor

FRAX 486

Potent p21-activated kinase (PAK) inhibitor; brain penetrant and orally bioavailable

BIX 02189

Selective MEK5 and ERK5 inhibitor

TC Mps1 12

Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor; orally active

GSK 2606414

Potent and selective PERK inhibitor; orally bioavailable

AZ 20

Potent and selective ATR kinase inhibitor; antitumor

AZD 7762 hydrochloride

Potent and selective ATP-competitive inhibitor of Chk1 and Chk2

PHT 427

Dual Akt and PDK1 inhibitor; antitumor

ML 786 dihydrochloride

Potent Raf kinase inhibitor; orally bioavailable

Senexin A

Cyclin-dependent kinase 8 (cdk8) inhibitor

XL 388

Potent and selective mTOR inhibitor; antitumor

PS 1145 dihydrochloride

Selective IKK inhibitor; orally active

Sign-up for new product e-alerts
divider line

Bio-Techne Events

Neuroscience 2014

Neuroscience 2014

November 15 - 19, 2014

Washington D.C., USA