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:
Product Name
TPCA-1, ≥95% (HPLC)
Quality Level
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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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
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