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T1452

Sigma-Aldrich

TPCA-1

≥95% (HPLC)

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C12H10FN3O2S
Numéro CAS:
507475-17-4
Poids moléculaire :
279.29
Numéro MDL:
MFCD09037541
Code UNSPSC :
12352200
ID de substance PubChem :
329826675
Nomenclature NACRES :
NA.77

Pureté

≥95% (HPLC)

Forme

powder

Couleur

white to light brown

Solubilité

DMSO: 5 mg/mL, clear

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne SMILES 

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)

Clé InChI

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.

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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

Notes préparatoires

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Équipement de protection individuelle

dust mask type N95 (US), Eyeshields, Gloves

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

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)
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
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
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
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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