TBBD

TBBD is a specific inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1; PRMT4) that selectively inhibits methylation at arginine 17 of histone H3 (H3R17); shows no significant effect on the HMTase activity of G9a, as well as on the HAT activity of p300/CBP-associated factor.(In Vitro):Ellagic acid is a potent CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM. Ellagic acid also blocks other kinases such as LYN, PKA, SYK, GSK3, FGR and CK1, with IC50s of 2.9, 3.5, 4.3, 7.5, 9.4 and 13.0 μM, respectively, and shows no obvious effects on DYRK1a, CSK, NPM-ALK, RET and FLT3 (IC50s > 40 μM). Ellagic acid (5-100 μM) shows inhibitory activities against Karpas299, SUDHL1, SR786, and FE-PD cell lines. Ellagic acid (10 μM) exhibits cytotoxic effects on MCF-7 cells after treatment of radiation. Ellagic acid (10 μM) in combination with Irradiation (IR) significantly abridges the capacity of MCF-7 cells to form colonies equated with individual treatments. Ellagic acid with IR also induces cell apoptosis, and facilitates the upregulation of pro-apopttotic Bax and downregulation of Bcl-2 in MCF-7 cells.\n(In Vivo):Ellagic acid (EA; 10 mg/kg/day; p.o., 14 days) strongly decreases MDA brain content by 17%, and reduces the levels of brain TNF-α by 42% in rats. Ellagic acid markedly increases the reduced brain contents of 5-HT (39%), dopamine (DA, 71%), and norepinephrine (NE, 77%). Ellagic acid (10 mg/kg, p.o., 14 days) causes decreased histopathological changes induced by Doxorubicin in rats.