T1452
TPCA-1
≥95% (HPLC), IκB kinase-2 (IKK-2) Inhibitor, powder
Synonyme(s) :
[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide
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A propos de cet article
Formule empirique (notation de Hill) :
C12H10FN3O2S
Numéro CAS:
Poids moléculaire :
279.29
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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Laissez-nous vous aiderNom du produit
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
Catégories apparentées
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.
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
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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
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
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
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
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