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| 规格： | 10 mM * 1 mL | 产品价格： | ￥1432.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥457.0 |
| 规格： | 5 mg | 产品价格： | ￥1100.0 |
| 规格： | 10 mg | 产品价格： | ￥1805.0 |
| 规格： | 25 mg | 产品价格： | ￥3000.0 |
| 规格： | 50 mg | 产品价格： | ￥4800.0 |
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GSK2033
CAS No. : 1221277-90-2
MCE 国际站：GSK2033
产品活性：GSK2033 是一种 LXR 拮抗剂，对于 LXRα 和 LXRβ 的 pIC50 值分别为 7 和 7.4。
研究领域：Metabolic Enzyme/Protease | Vitamin D Related/Nuclear Receptor
作用靶点：LXR
In Vitro: GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively. GSK2033 dose-dependently suppresses basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC50s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppresses the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC50s of 52 nM for LXRα and 10 nM for LXRβ. GSK2033 also suppresses the expression of both of fatty acid synthase (FASN) and SREBP1.
In Vivo: One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels.? Plasma triglyceride levels are also unaffected by treatment with GSK2033.
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文献和实验Inhibition of Glycogen Synthase Kinase-3 Methods in Molecular Biology v468. chapter 5 Abstract There are two homologous forms of glycogen synthase kinase (GSK)-3, GSK-3a and GSK-3b, whichplay overlapping roles in the regulation of Wnt
v468. chapter 4 WNT 细胞通路 检测细胞GSK3活性与表达水平
a pseudo-substrate and binds to the phosphate-binding pocketon GSK3, preventing interaction with primed substrates (8) . Phosphorylation at this site is mediated by members of the AGCfamily of kinases (e.g. PKB, PKC, p70S6K, and p90RSK) andcommonly
(Simultaneous inhibition of GSK3alpha and GSK3beta using hairpin siRNA expression vectors. Mol Ther. 2003 Feb;7(2):228-36. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=12597911&query_hl=7)等人报道虽然加长shRNA可以改善原本无效的19bp
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