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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:
Molecular Weight:
279.29
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
powder
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Product Name

TPCA-1, ≥95% (HPLC)

Quality Segment

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

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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