| HG-9-91-01Pan-SIK (salt-inducible kinases) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.07%
- COA (Certificate Of Analysis)
- HPLC
- MS(Mass Spectrometry)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
Related Biological Data
Related Biological Data
| Cell experiment [1]: | |
Cell lines | Macrophages |
Preparation method | Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 1 h |
Applications | HG-9-91-01increases LPS-stimulated IL-10 production and markedly inhibits proinflammatory cytokine secretion even when WT SIK2 is expressed to the same level. In addition, CRTC3 is required for HG-9-91-01 to enhance IL-10 production in LPS-stimulated primary mouse macrophages. |
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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| Cas No. | 1456858-58-4 | SDF | Download SDF |
| Synonyms | N/A | ||
| 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 | ||
| 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 | ||
| Formula | C32H37N7O3 | M.Wt | 567.68 |
| Solubility | ≥56.8mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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请赐教！
荚膜（capsule）是某些细菌在生长繁殖过程中分泌的一层黏液性物质，包围在细胞壁外，通常这种黏液层厚度小于0.2μm，成分是多糖或多肽，只有在营养丰富时或在动物体内，细菌才产生这种半抗原性质的黏液性物质。它具有保护菌体免受巨噬细胞等的捕捉和吞噬，因而具有抗吞噬抗消化、侵袭力强、与致病性关系密切等特点。像肺炎球菌、炭疽杆菌等都有这类荚膜。有些细菌的荚膜层较薄，小于0.2μm，称为微荚。
像链球菌的M蛋白、伤寒杆菌的Vi抗原、大肠杆菌的K抗原等都属于这类微荚膜。
颗粒型抗原,除了有细菌、红细胞、螺旋体等天然颗粒型抗原,还有吸附有可溶性抗原的非免疫相关颗粒.
颗粒性抗原光镜下可见，比如细菌性抗原、红细胞抗原等；而可溶性抗原在光镜下不可见，如组织浸出液、细菌毒素、蛋白质分子等。
它们不等同于完全抗原和不完全抗原。完全抗原具有免疫原性和抗原性，而不完全抗原只具有抗原性。完全抗原可以是颗粒性抗原，亦可是可溶性抗原，而不完全抗原一般只能是可溶性抗原，不会是颗粒性抗原。
若已进入细胞内。则先由巨噬细胞吞噬降解。并形成抗原-MHC复合体传送到表面。被辅助性T淋巴细胞识别和效应T淋巴细胞识别后。效应T淋巴细胞被激活。分解靶细胞。然后再由效应B细胞分泌的抗体进一步消灭病毒。
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