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T1452

TPCA-1

Name: TPCA-1
Brand: SIGMA

≥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

Assay:

≥95% (HPLC)

Form:

powder

Quality level:

100

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Properties

Product Name

TPCA-1, ≥95% (HPLC)

Quality Level

100

assay

≥95% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: 5 mg/mL, clear

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

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

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)

InChI key

SAYGKHKXGCPTLX-UHFFFAOYSA-N

Description

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

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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)

IkappaB kinase-2-independent and -dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic.

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

Activation of signal transducer and activator of transcription 3 (STAT3) signaling in EGFR mutant non-small-cell lung cancer (NSCLC).

Carles Codony-Servat et al.

Oncotarget, 8(29), 47305-47316 (2017-05-19)

Gefitinib, erlotinib or afatinib are the current treatment for non-small-cell lung cancer (NSCLC) harboring an activating mutation of the epidermal growth factor receptor (EGFR), but less than 5% of patients achieve a complete response and the median progression-free survival is

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Global Trade Item Number

SKU	GTIN
T1452-1MG	04061826133163
T1452-5MG	04061832452555