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Merck

T1452

TPCA-1

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C12H10FN3O2S
CAS Number:
507475-17-4
Molecular Weight:
279.29
UNSPSC Code:
12352200
PubChem Substance ID:
329826675
NACRES:
NA.77
MDL number:
MFCD09037541

Key Documents

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Product Name

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

100

Related Categories

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

T1452-BULK: + T1452-VAR: + T1452-5MG: + T1452-1MG:

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Certificates of Analysis (COA)

Lot/Batch Number
0000463008
0000463008
0000158500
0000109522

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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
Galangin Abrogates Ovalbumin-Induced Airway Inflammation via Negative Regulation of NF-B.
Zha, W. J., et al.
Evidence-Based Complementary and Alternative Medicine : ECAM, 2013, doi:10-doi:10 (2013)
Ines Tagoug et al.
PloS one, 6(7), e22641-e22641 (2011-07-30)
Multiple myeloma (MM) is a B cell neoplasm characterized by bone marrow infiltration with malignant plasma cells. IGF-1 signalling has been explored as a therapeutic target in this disease. We analyzed the effect of the IKK2 inhibitor AS602868, in combination
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
Y Gao et al.
Oncogenesis, 6(9), e383-e383 (2017-09-26)
Clinical and experimental evidence indicates that macrophages could promote solid-tumor progression and metastasis. However, the mechanisms underlying this process remain unclear. Here we show that yes-associated protein 1 (YAP1), a transcriptional regulator that controls tissue growth and regeneration, has an
View All Related Papers

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