S80473 |
C-DIM12 |
源叶(MedMol) | 98% |
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- 产品描述: C-DIM12 induced expression of Nurr1-regulated genes. C-DIM12 increased expression of transfected human Nurr1, induced Nurr1 protein expression in primary dopaminergic neurons and enhanced neuronal survival from exposure to 6-OHDA.
- 靶点: Apoptosis
- 体外研究:
C-DIM12 induces Nurr1 and DA gene expression in cell lines and primary neurons[3]. C-DIM12 suppresses astrocyte inflammatory signaling in vitro. C-DIM12 inhibits lipopolysaccharide (LPS)–induced expression of NF-κB-regulated genes in BV-2 microglia including nitric oxide synthase (NOS2), interleukin-6 (IL-6), and chemokine (C-C motif) ligand 2 (CCL2), and the effects were attenuated by Nurr1-RNA interference. Additionally, C-DIM12 decreased NF-κB activation in NF-κB–GFP (green fluorescent protein) reporter cells and enhanced nuclear translocation of Nurr1 primary microglia. C-DIM12 decreases lipopolysaccharide-induced p65 binding to the NOS2 promoter and concurrently enhanced binding of Nurr1 to the p65-binding site. C-DIM12 also stabilized binding of the Corepressor for Repressor Element 1 Silencing Transcription Factor (CoREST) and the Nuclear Receptor Corepressor 2 (NCOR2)。
- 体内研究:
C-DIM12 has the neuroprotective activity in MPTPp-treated mice。
- 细胞实验: NF-κB–GFP HEK cells are exposed to 30 ng/ml of TNFα in the presence of 100 μM C-DIM12 for up to 24 hours. C-DIM12 is efficient at blocking NF-κB–GFP expression in the NF-κB–GFP HEK cells after TNFα treatment, displaying a statistically significant reduction in total GFP fluorescence per cell.(Only for Reference)
- 参考文献:
1. Hammond SL, Safe S, Tjalkens RB. A novel synthetic activator of Nurr1 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro. Neurosci Lett. 2015 Oct 21;607:83-9. doi: 10.1016/j.neulet.2015.09.015. Epub 2015 Sep 14. PubMed PMID: 26383113; PubMed Central PMCID: PMC4631643.
2. De Miranda BR, Popichak KA, Hammond SL, Jorgensen BA, Phillips AT, Safe S, Tjalkens RB. The Nurr1 Activator 1,1-Bis(3'-Indolyl)-1-(p-Chlorophenyl)Methane Blocks Inflammatory Gene Expression in BV-2 Microglial Cells by Inhibiting Nuclear Factor κB. Mol Pharmacol. 2015 Jun;87(6):1021-34. doi: 10.1124/mol.114.095398. Epub 2015 Apr 9. PubMed PMID: 25858541; PubMed Central PMCID: PMC4429718.
3. De Miranda BR, Popichak KA, Hammond SL, Miller JA, Safe S, Tjalkens RB. Novel para-phenyl substituted diindolylmethanes protect against MPTP neurotoxicity and suppress glial activation in a mouse model of Parkinson's disease. Toxicol Sci. 2015 Feb;143(2):360-73. doi: 10.1093/toxsci/kfu236. Epub 2014 Nov 17. PubMed PMID: 25406165; PubMed Central PMCID: PMC4306720.
- 溶解性: Soluble in DMSO、Ethanol
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.802 ml 14.012 ml 28.023 ml 5 mM 0.56 ml 2.802 ml 5.605 ml 10 mM 0.28 ml 1.401 ml 2.802 ml 50 mM 0.056 ml 0.28 ml 0.56 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)