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T1452

TPCA-1

Name: TPCA-1
Brand: SIGMA

≥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:

507475-17-4

分子量:

279.29

UNSPSC Code:

12352200

PubChem Substance ID:

329826675

NACRES:

NA.77

MDL number:

MFCD09037541

Assay:

≥95% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

TPCA-1, ≥95% (HPLC)

Quality Level

100

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

说明

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

0000463008

0000158500

0000109522

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Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation.

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

TNFα-YAP/p65-HK2 axis mediates breast cancer cell migration.

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

Inhibition of IGF-1 signalling enhances the apoptotic effect of AS602868, an IKK2 inhibitor, in multiple myeloma cell lines.

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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