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Anacardic Acid p300/CBP inhibitor

Name: Anacardic Acid
Brand: Selleck Chemicals
SKU: S7582
Availability: InStock
Rating: 5 (24 reviews)

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.

Chemical Structure

Molecular Weight: 348.52

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Quality Control

Batch: Purity: 99.72%

99.72

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Other p300/CBP Inhibitors	Inobrodib (CCS-1477) A-485 Curcumin SGC-CBP30 CPI-637 E7386 I-CBP112 GNE-049 Histone Acetyltransferase Inhibitor II TTK21

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
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

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (197.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 69 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.250mg/ml (12.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	348.52	Formula	C₂₂H₃₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	16611-84-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	Tip60 (Cell-free assay) PCAF (Cell-free assay) 5 μM p300/CBP (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. 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. 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.
Kinase Assay	HAT and HDAC Activity Assays
Kinase Assay	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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12624111/ [2] https://pubmed.ncbi.nlm.nih.gov/16844118/ [3] https://pubmed.ncbi.nlm.nih.gov/25101666/ [4] https://pubmed.ncbi.nlm.nih.gov/22103711/

Applications

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

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Handling Instructions

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