T1452
TPCA-1
≥95% (HPLC), IκB kinase-2 (IKK-2) Inhibitor, powder
别名:
[5-（对-氟苯基）-2-脲基]噻吩-3-甲酰胺
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关于此项目
经验公式（希尔记法）:
C12H10FN3O2S
化学文摘社编号:
分子量:
279.29
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
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
Application
TPCA-1已用于研究其在RPMI8226和LP1细胞系中的细胞毒性作用。它还可作为培养基补充剂，用于从人气道平滑肌细胞中提取的核蛋白组分。
Biochem/physiol Actions
IKK-2抑制剂
TPCA-1是人IκB激酶-2（IKK-2）的一种有效选择性抑制剂，对于IKK-2的IC50 = 17.9 nM，而相比之下IKK-1为400 nm。它已用于研究IKK-2的抑制以防止炎症介质在关节炎和气道炎症动物模型中的释放。
Features and Benefits
该化合物由 GlaxoSmithKline 开发。想要浏览其他由制药公司开发的化合物以及已批准药物/候选药物清单，请单击此处。
Preparation Note
TPCA-1可以大于或等于10 mg/ml的浓度溶于DMSO。它不可溶于水。
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
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
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
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
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
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