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CAS No.: 507475-17-4

TPCA-1 Catalog No. CSN13432

Synonyms: GW683965;IKK2 Inhibitor IV

TPCA-1 is a selective and potent IKK-β inhibitor with IC50 value of 17.9 nM.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 IKK2

IC50:17.9nM
描述In a time-resolved fluorescence resonance energy transfer assay, TPCA-1 inhibits human IKK-2 activity with an IC50 of 17.9 nM. In addition, TPCA-1 is demonstrated to be ATP-competitive. Besides, TPCA-1 exhibits IC50 values of 400 nM and 3600 nM against IKK-1 and JNK3, respectively. TPCA-1 inhibits the production of TNF-α, IL-6, and IL-8 in a concentration-dependent manner, exhibiting IC50 values of 170, 290, and 320 nM, respectively. TPCA-1 inhibits glioma cell proliferation, as well as TNF-induced RelA (p65) nuclear translocation and NFκB-dependent IL8 gene expression. Importantly, TPCA-1 inhibits IFN-induced gene expression, completely suppressing MX1 and GBP1 gene expression, while having only a minor effect on ISG15 expression.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
C57BL/6 mouse BMDM cells	-	Cytotoxicity assay	24 h	Cytotoxicity against C57BL/6 mouse BMDM cells assessed as LDH release after 24 hrs	22533790
C57BL/6 mouse BMDM cells	0.5 μM	Function assay	1 h	Antiinflammatory activity in C57BL/6 mouse BMDM cells assessed as inhibition of LPS-stimulated TNFalpha production at 0.5 uM pretreated for 1 hr before LPS challenge after 8 to 24 hrs by immunoassay	22533790

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5805 mL
- 17.9025 mL
- 35.8051 mL
- 5 mM
- 0.7161 mL
- 3.5805 mL
- 7.1610 mL
- 10 mM
- 0.3581 mL
- 1.7903 mL
- 3.5805 mL

技术信息

CAS号

507475-17-4

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H10FN3O2S

运输

蓝冰

分子量

279.29

别名

GW683965;IKK2 Inhibitor IV

溶解度

DMSO	235.0 mg/mL (841.4 mM)
Water	insoluble

动物实验配方

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TPCA-1 Catalog No. CSN13432

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