Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

p300 HAT:8.5 μM, PCAF(p300/CREB-binding protein-associated factor):5 μM

Anacardic acid is an inhibitor of several Clinicalally targeted enzymes such as HATs, NF-kB, LOX-1, xanthine oxidase, tyrosinase, and ureases. Anacardic acid is also an effective inhibitor of Tip60 in vitro. It inhibits the Tip60-dependent acetylation and activation of the ATM protein kinase in HeLa cells and sensitizes the cells to the cytotoxic effects of radiation.

Anacardic acid decreases over-expression of Gata4, α-MHC, and cTnT in fetal mouse hearts exposed to ethanol. Anacardic acid inhibits binding of PCAF, P300 to the promoter of Gata4.

HAT and HDAC Activity Assays :After homogenization of cardiac tissues, nucleoproteins are extracted using a Nuclear Extract Kit according to the manufacturer's instructions. HAT and HDAC activities of the nuclear protein extracts are determined using a colorimetric assay included in the HAT and HDAC assay kits.

HeLa and 293T cells are grown in Dulbecco's modified Eagle's medium/10% fetal calf serum. SQ20B and SCC35 squamous cell carcinoma cell lines are cultured in modified eagles medium/10% fetal calf serum. For anacardic acid (EMD Biosciences, CA) exposure, cells are preincubated with anacardic acid (0-100 μM) for 40 min, irradiated, then allowed to recover for 4 h. Cells are then switched to fresh media and allowed to grow for 10 days.

Animal Models: 9 to 11 week old Kunming mice. Formulation: Dissolved in DMSO,co-injected with ethanol. Dosages: 0,1.25,2.5,5,10 mg/kg. Administration: i.p.