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Merck
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T1452

Sigma-Aldrich

TPCA-1

≥95% (HPLC)

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C12H10FN3O2S
Número de CAS:
507475-17-4
Peso molecular:
279.29
Número MDL:
MFCD09037541
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
329826675
NACRES:
NA.77

Nivel de calidad

100

Ensayo

≥95% (HPLC)

Formulario

powder

color

white to light brown

solubilidad

DMSO: 5 mg/mL, clear

emisor

GlaxoSmithKline

temp. de almacenamiento

2-8°C

cadena 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)

Clave InChI

SAYGKHKXGCPTLX-UHFFFAOYSA-N

Aplicación

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.

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

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

Nota de preparación

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Equipo de protección personal

dust mask type N95 (US), Eyeshields, Gloves

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Certificados de análisis (COA)

Lot/Batch Number
075M4703V
081M4617V
067K46084
067K46083

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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)
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
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
Lauren D Aarreberg et al.
mBio, 9(2) (2018-03-22)
Induction of interferon beta (IFN-β), IFN-stimulated genes (ISGs), and inflammatory responses is critical for control of viral infection. We recently identified an essential linkage of stimulation of the inflammatory cytokine interleukin-1β (IL-1β) and induction of ISGs that function as host
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