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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEProtosappanin ACat. No.: HY-113573CAS No.: 102036-28-2Synonyms: PTA分式: CHO分量: 272.25作靶點: JAK; STAT作通路: Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt儲存式: 4C, sealed storage, away from moisture and light* In solvent : -80C, 6 mon

2、ths; -20C, 1 month (sealedstorage, away from moisture and light)BIOLOGICAL ACTIVITY物活性 Protosappanin A (PTA),種免疫制劑, 從 Caesalpinia sappan L 中分離得到的種主要聯(lián)苯化合物,通過下調(diào) JAK2 和 STAT3 的磷酸化,抑制 JAK2/STAT3 依賴的炎癥通路。IC50 & Target JAK2 STAT3體外研究Protosappanin A (PTA: 12.5, 25, 50 M, 24 hours) significantly inhibits th

3、e production of TNF- and IL-1 inLPS-activated BV2 microglia. And the mRNA expressions of IL-6, IL-1, and MCP-1 are reduced by PTA in adose-dependent manner in BV2 microglial cell line 1.Protosappanin A (PTA: 12.5, 25, 50 M, 24 hours) suppresses JAK2/STAT3-dependent inflammationpathway through down-r

4、egulating the phosphorylation of JAK2 and STAT3, as well as STAT3 nucleartranslocation against LPS treatment 1.Protosappanin A (PTA: 12.5, 25, 50 M, 24 hours) shows obvious effect on disturbing the interaction oftransmembrane protein CD14 with Toll-like receptor-4, resulting in the inhibition of NF-

5、B-dependentoxidative and nitrative stress in LPS-induced BV2 microglia 2.Western Blot Analysis 1Cell Line: Murine BV2 microglial cell line.Concentration: 12.5, 25, 50 M.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEIncubation Time: 24 hours.Result: Inhibits the releases of NO, TNF- and IL-1 in LP

6、S-induced BV2 cells.Attenuated IL-6, IL-1 and MCP-1 gene expressions in the LPS-induced BV2 cells.Suppressed JAK2/STAT3 pathway activation in the LPS-induced BV2 cells.REFERENCES1. Wang LC, et al. Protosappanin A exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccha

7、ride-inducedBV2 microglia. Chin J Nat Med. 2017 Sep;15(9):674-679.2. Zeng KW, et al. Protosappanin A inhibits oxidative and nitrative stress via interfering the interaction of transmembrane protein CD14 withToll-like receptor-4 in lipopolysaccharide-induced BV-2 microglia. Int Immunopharmacol, 2012, 14(4): 558- 569.McePdfHeightCaution: Product has not been fully validated for medical applications.For research

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