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
CAS Number:
分子量:
279.29
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
Product Name
TPCA-1, ≥95% (HPLC)
质量水平
方案
≥95% (HPLC)
表单
powder
颜色
white to light brown
溶解性
DMSO: 5 mg/mL, clear
创始人
GlaxoSmithKline
储存温度
2-8°C
SMILES字符串
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
应用
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。
生化/生理作用
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。
特点和优势
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。
制备说明
TPCA-1可以大于或等于10 mg/ml的浓度溶于DMSO。它不可溶于水。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
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
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
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