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HG-9-91-01

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Catalog No.
B1052
Pan-SIK (salt-inducible kinases) 抑制剂
组合的产品项目
规格价格库存 数量
2mg
¥ 1,620.00
现货
5mg
¥ 2,430.00
现货
10mg
¥ 3,690.00
现货
50mg
¥ 8,750.00
现货
100mg
¥ 13,610.00
现货

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Background

HG-9-91-01 is a pan-SIK (salt-inducible kinases) inhibitor with IC50 values of 0.92nM, 6.6nM and 9.6nM for SIK1, SIK2, SIK3, respectively [1].

SIKs restrict the formation of regulatory macrophages. The inhibition of these enzymes is thought to have potential for treating inflammatory and autoimmune diseases. HG-9-91-01 potently inhibits SIKs through targeting both the ATP-binding site and the small hydrophobic pocket. It is reported that, besides SIKs, HG-9-91-01 also inhibits various protein tyrosine kinases such as Src, BTK, FGF and Ephrin receptors. But other AMPK-related kinase subfamily members are not sensitive to HG-9-91-01. HG-9-91-01 can promote LPS-stimulated IL-10 production, CREB-dependent gene transcription, inhibit proinflammatory cytokine secretion and induce the expression of regulatory macrophage markers [1].

References:
[1] Clark K, MacKenzie K F, Petkevicius K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proceedings of the National Academy of Sciences, 2012, 109(42): 16986-16991.

文献引用

1. Wang Z, Ma J, Met al. "Quantitative phosphoproteomic analysis of the molecular substrates of sleep need." Nature. 2018 Jun;558(7710):435-439. PMID:29899451
2. Abend A, Shkedi O, et al. "Salt-inducible kinase induces cytoplasmic histone deacetylase 4 to promote vascular calcification." EMBO Rep.2017 Jul;18(7):1166-1185. PMID:28588072

Chemical Properties

StorageStore at -20°C
M.Wt567.68
Cas No.1456858-58-4
FormulaC32H37N7O3
Solubility≥56.8mg/mL in DMSO
Chemical Name(Z)-N-(2,4-dimethoxyphenyl)-N'-(2,6-dimethylphenyl)-N-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamimidic acid
SDFDownload SDF
Canonical SMILESCC1=C(/N=C(O)/N(C2=NC=NC(NC3=CC=C(N4CCN(CC4)C)C=C3)=C2)C5=C(OC)C=C(OC)C=C5)C(C)=CC=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

巨噬细胞

制备方法

溶解度有限,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

1 h

实验结果

HG-9-91-01增加LPS刺激的IL-10生成,显著抑制促炎细胞因子的分泌,即使WT SIK2表达到相同水平时也有此种效果。此外,HG-9-91-01需要CRTC3以增强LPS刺激的原代小鼠巨噬细胞中的IL-10生成。

References:

1. Clark K, MacKenzie KF, Petkevicius K et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.

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化学结构

HG-9-91-01

相关生物数据

HG-9-91-01

相关生物数据

HG-9-91-01