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Beschreibung

A cell-permeable and water soluble hydrazinobenzoylcurcumin (HBC) compound that acts as a selective, reversible and mixed mode inhibitor of p300/CBP and PCAF histone acetyltransferases (IC50 <= 25 and 50 µ,M, respectively) with minimal activity towards other histone modifying enzymes like, G9a, CARM1, HDAC1, SIRT2 and TIP60 (IC50 >100 µ,M). Blocks the autoacetylation of p300 and PCAF and histone acetylation, downregulates cyclin E expression and induces senescence-like growth arrest at 100 µ,M in KB cells. Further, suppresses tumor growth in xenograft oral tumor nude mouse model (100 mg/kg, i.p., b.i.d.) and reduces H3K14 and H3K9 acetylation levels. Reported to potently inhibit bFGF-induced bovine aortic endothelial cells (BAECs) invasion and tube formation with an IC50 of 0.93 µ,M and binds to Ca2+/calmodulin with high-affinity (Kd = 8.11 µ,M) and antagonize its functions in HCT15 cells.