Anacardic Acid Histone Acetyltransferase inhibitor

Cat.No.S7582

Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity, prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
Anacardic Acid Histone Acetyltransferase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 348.52

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hi5 cells Function assay Non-competitive inhibition of human recombinant His-GST tagged VCP expressed in baculovirus infected Hi5 cells
HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by luciferase reporter gene assay, IC50=0.38 μM
Hi5 cells Function assay Inhibition of human recombinant His-GST tagged VCP expressed in baculovirus infected Hi5 cells assessed as ADP formation incubated for 20 mins proir to substrate addition measured after 90 mins by NADH coupled assay, IC50=0.024 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 348.52 Formula

C22H36O3

Storage (From the date of receipt)
CAS No. 16611-84-0 Download SDF Storage of Stock Solutions

Synonyms 6-pentadecylsalicylic Acid Smiles CCCCCCCCCCCCCCCC1=C(C(=CC=C1)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 69 mg/mL ( (197.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 69 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Tip60 [2]
(Cell-free assay)
PCAF [1]
(Cell-free assay)
5 μM
p300/CBP [1]
(Cell-free assay)
8.5 μM
In vitro
Anacardic acid is found to be a common inhibitor of several clinically targeted enzymes such as NFkB kinase, histone acetyltransferase (HATs), lipoxygenase (LOX-1), xanthine oxidase, tyrosinase and ureases[4]. Anacardic acid is also an efficient 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[2]. Anacardic acid can effectively prevent cell damage induced by H2O2 because this can be converted to ROS, hydroxyl radicals, in the presence of metal ions[4].
Kinase Assay
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.
In vivo
Anacardic acid attenuates over-expression of Gata4, α-MHC and cTnT in fetal mouse hearts exposed to ethanol. Anacardic acid inhibits binding of P300, PCAF to the promoter of Gata4[3].
References

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell viability S7582-viability1 30210681
Western blot GRP78 / Hsp70 / CDK4 E-cadherin / Vimentin / MMP-9 ErbB2 S7582-WB1 30210681

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