HG-9-91-01
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
HG-9-91-01是一种SIK（盐诱导激酶）抑制剂，作用于SIK1、SIK2和SIK3，IC50值分别为0.92nM、6.6nM和9.6nM[1]。
SIKs限制调节性巨噬细胞的形成。这些酶的抑制作用被认为可用于治疗炎症和自身免疫疾病。HG-9-91-01靶向结合ATP结合位点和小的疏水口袋，从而有效地抑制SIKs。据报道，除了SIKs，HG-9-91-01也可以抑制多种蛋白酪氨酸激酶，例如Src、BTK、FGF和Ephrin 受体。然而，其它AMPK相关激酶亚家族的成员对HG-9-91-01不敏感。HG-9-91-01可以促进LPS刺激的IL-10的生产和CREB-依赖性基因转录，抑制促炎细胞因子的分泌，诱导调节性巨噬细胞标记的表达[1]。
参考文献：
[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.
- 1. Caterina Iorio, Jillian L. Rourke, Met al. "Silencing the G-protein coupled receptor 3-salt inducible kinase 2 pathway promotes human β cell proliferation." Commun Biol. 2021 Jul 23;4(1):907. PMID:34302056
- 2. 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
- 3. 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
| Storage | Store at -20°C |
| M.Wt | 567.68 |
| Cas No. | 1456858-58-4 |
| Formula | C32H37N7O3 |
| Solubility | ≥56.8 mg/mL in DMSO; ≥27.3 mg/mL in EtOH; ≥6.35 mg/mL in H2O with ultrasonic |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1=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 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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。 |
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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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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
相关生物数据
