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Merck

T1452

TPCA-1

≥95% (HPLC), IκB kinase-2 (IKK-2) Inhibitor, powder

Sinónimos:

[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C12H10FN3O2S
Número CAS:
Peso molecular:
279.29
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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Nombre del producto

TPCA-1, ≥95% (HPLC)

SMILES string

NC(=O)Nc1sc(cc1C(N)=O)-c2ccc(F)cc2

InChI key

SAYGKHKXGCPTLX-UHFFFAOYSA-N

InChI

1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18)

assay

≥95% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: 5 mg/mL, clear

originator

GlaxoSmithKline

storage temp.

2-8°C

Quality Level

Categorías relacionadas

Application

TPCA-1 has been used to study its cytotoxic effects in RPMI8226 and LP1 cell lines. It has also been used as a culture media supplement for nuclear protein fractions extracted from human airway smooth muscle cells.

Biochem/physiol Actions

IKK-2 Inhibitor
TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Preparation Note

TPCA-1 is soluble in DMSO at a concentration that is greater than or equal to 10 mg/ml. It is insoluble in water.

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves


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Evidence-Based Complementary and Alternative Medicine : ECAM, 2013, doi:10-doi:10 (2013)
Mark A Birrell et al.
Molecular pharmacology, 69(6), 1791-1800 (2006-03-07)
Nuclear factor kappaB (NF-kappaB) is a transcription factor believed to be central in the expression of numerous inflammatory genes and the pathogenesis of many respiratory diseases. We have previously demonstrated increased NF-kappaB pathway activation in a steroid-sensitive animal model of
Ines Tagoug et al.
PloS one, 6(7), e22641-e22641 (2011-07-30)
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Patricia L Podolin et al.
The Journal of pharmacology and experimental therapeutics, 312(1), 373-381 (2004-08-19)
Demonstration that IkappaB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-kappaB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-alpha and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment
Alice Borghi et al.
Biochemical pharmacology, 153, 292-298 (2018-01-30)
Tumor Necrosis Factor (TNF) is a proinflammatory cytokine that elicits its action by binding to two cell surface TNF receptors (TNFR), TNFR1 and TNFR2, which are expressed by many different cell types. Stimulation of TNFR1 activates canonical NF-κB signaling, leading

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