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CAS No.: 354812-17-2

SC-514 Catalog No. CSN16524

Synonyms: GK 01140

SC514 is a potent, reversible, ATP-competitive and highly selective IKK-β(IKK-2) inhibitor with IC50 value ranging in 3-12 µM.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述The I kappaB kinase (IKK) complex is involved in transcriptional activation by phosphorylating the inhibitory molecule I kappaB alpha, a modification that triggers its subsequent degradation, enabling activation of nuclear factor kappa B (NF-kappaB)^[3]. IkappaB kinases (IKK) and IKK-related kinases play critical roles in regulating the immune response through nuclear factor-kappaB and IFN regulatory factor-dependent signaling transduction cascades^[4].Diabetic rats exhibited significantly decreased levels of GHSR-1a and protein phosphatase 1 (PP1) in the hippocampus and increased activation of the IKK/NF-κB/BACE1 pathway. Chronic ghrelin administration upregulated hippocampal PP1 expression, suppressed IKK/NF-κB/BACE1 mediated Aβ production, and improved cognition in STZ-induced diabetic rats^[5]. SC-514 is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression. SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer and IKK-2 homodimer similarly. IKK-2 inhibition by SC-514 is selective, reversible, and competitive with ATP. SC-514 inhibits transcription of NF-kappa B-dependent genes in IL-1 beta-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent manner.^[6].SC514 also demonstrated ability to inhibit COX2 protein responses and a broad down-regulatory effect on uterine cell inflammatory gene expression^[7].
参考文献

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
- 4.4583 mL
- 22.2913 mL
- 44.5826 mL
- 5 mM
- 0.8917 mL
- 4.4583 mL
- 8.9165 mL
- 10 mM
- 0.4458 mL
- 2.2291 mL
- 4.4583 mL

技术信息

CAS号

354812-17-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H8N2OS2

运输

蓝冰

分子量

224.30

别名

GK 01140

溶解度

DMSO	225.0 mg/mL (1003.1 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water

4 mg/mL

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