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SC-514

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Chemical Structure| 354812-17-2 同义名 : GK 01140
CAS号 : 354812-17-2
货号 : A499215
分子式 : C9H8N2OS2
纯度 : 98%
分子量 : 224.303
MDL号 : MFCD00206459
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(222.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+2% Tween 80+water 4 mg/mL

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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.46mL

0.89mL

0.45mL

22.29mL

4.46mL

2.23mL

44.58mL

8.92mL

4.46mL
参考文献

[1]Jeong SJ, Pise-Masison CA, et al. A novel NF-kappaB pathway involving IKKbeta and p65/RelA Ser-536 phosphorylation results in p53 Inhibition in the absence of NF-kappaB transcriptional activity. J Biol Chem. 2005 Mar 18;280(11):10326-32.

[2]Kishore N, Sommers C, et al. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71.

[3] Alain Chariot,et al. The NF-kappaB-independent functions of IKK subunits in immunity and cancer. Trends Cell Biol. 2009 Aug;19(8):404-13.

[4]Dung-Fang Lee,et al. Advances in targeting IKK and IKK-related kinases for cancer therapy. Clin Cancer Res. 2008 Sep 15;14(18):5656-62.

[5]Lou-Yan Ma,et al. Chronic ghrelin administration suppresses IKK/NF-κB/BACE1 mediated Aβ production in primary neurons and improves cognitive function via upregulation of PP1 in STZ-diabetic rats. Neurobiol Learn Mem. 2020 Mar;169:107155.

[6]Nandini Kishore,et al. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71.

[7] Leo R I Gurney,et al. Inhibition of Inflammatory Changes in Human Myometrial Cells by Cell Penetrating Peptide and Small Molecule Inhibitors of NFκB. Front Immunol. 2018 Dec 20;9:2966.