Tanshindiol C 

Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ 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^[1][2].

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^[1].
Tanshindiol C inhibits both wild-type and A667G mutant (K_i value of 176 nM) EZH2 activity with similar potencies^[2].
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 GI₅₀ values of 1.5 μM, 9.5 μM, 10.6 μM, 4 μM, 6 μM, 5.7 μM and 4.2 μM, respectively^[2].
Tanshindiol C (1-5 μM; 72 hours) induces accumulation of Pfeiffer cells in sub-G1 phase, which indicates cells in late apoptosis and necrosis^[2].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

312.32

C₁₈H₁₆O₅

97465-71-9

Solid

Brown to red

O=C(C1=C2C=CC3=C1CC[C@@H](O)[C@@]3(O)C)C(C4=C2OC=C4C)=O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Yuyu Yang, et al. Tanshindiol C inhibits oxidized low-density lipoprotein induced macrophage foam cell formation via a peroxiredoxin 1 dependent pathway. Biochim Biophys Acta Mol Basis Dis. 2018 Mar;1864(3):882-890.  [Content Brief]

  [2]. Jimin Woo, et al. Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2486-92.  [Content Brief]