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

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

RSVA 405

AMPK activator

Atiprimod dihydrochloride

JAK2 inhibitor

Sign-up for new product e-alerts
divider line

Bio-Techne Events

Annual Meeting of the Japan Neuroscience Society

Annual Meeting of the Japan Neuroscience Society

September 11 - 13, 2014

Yokohama, Japan