Tanshindiol C is a S-adenosylmethionine-competitive EZH2 ( Histone Methyltransferase ) inhibitor with an IC 50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research In Vitro Tanshindiol C (1-10 μM; for 24 h) activates Nrf2 and upregulates Prdx1 expression and mRNA levels in macrophages. Tanshindiol C protects macrophages from oxidized low-density lipoprotein (oxLDL) induced foam cell formation via activation of Prdx1/ABCA1 signaling. Tanshindiol C inhibits both wild-type and A667G mutant (K i value of 176 nM) EZH2 activity with similar potencies. Tanshindiol C inhibits growth of the cell lines such as Pfeiffer, U-2932 and Daudi (lymphoma), PC3 (prostate cancer), T98G and U87MG (glioma), and A549 (lung cancer), with GI 50 values of 1.5 μM, 9.5 μM, 10.6 μM, 4 μM, 6 μM, 5.7 μM and 4.2 μM, respectively. Tanshindiol C (1-5 μM; 72 hours) induces accumulation of Pfeiffer cells in sub-G1 phase, which indicates cells in late apoptosis and necrosis. Tanshindiol C (1-3 μM; 72 hours) increases protein levels of the important apoptosis related protein markers, cleaved caspase-3, caspase-7 and poly ADP-ribose polymerase (PRAP) in the cells.Tanshindiol C significantly decreases the levels of H3K27me3 in cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: RAW264.7 cells Concentration: 1 μM, 3 μM, 10 μM Incubation Time: 24 h Result: Upregulated the Nrf2 and Prdx1 mRNA levels. Western Blot AnalysisCell Line: Mouse peritoneal macrophages Concentration: 1 μM, 3 μM, 10 μM Incubation Time: 24 h Result: Activated Nrf2 and upregulated Prdx1 expression in macrophages. Cell Cycle AnalysisCell Line: Pfeiffer cells Concentration: 1 μM, 2.5 μM and 5 μM Incubation Time: 72 hours Result: Induced accumulation of Pfeiffer cells in sub-G1 phase. Western Blot AnalysisCell Line: Pfeiffer cells Concentration: 1 μM, 3 μM Incubation Time: 72 hours Result: The levels of H3K27me3 was significantly decreased in the cells. Form:Solid IC50& Target:EZH2|0.55 μM (IC|50|)|SIRT1
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Tanshindiol C
CAS number：97465-71-9 molecular formula：C18H16O5
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| Chinese alias | 丹参二醇C | ||
| English alias | - | ||
| CAS number | 97465-71-9 | molecular formula | C18H16O5 |
| molecular weight | 312.32 g/mol | Exact mass | ≥98% |
| PSA | 87.700 Ų | logp | 1.200 |
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