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RG108 DNA Methyltransferase inhibitor

Name: RG108
Brand: Selleck Chemicals
SKU: S2821
Availability: InStock
Rating: 5 (29 reviews)

Cat.No.S2821

RG108 (N-Phthalyl-L-tryptophan) is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, and this compound does not cause trapping of covalent enzymes.

Chemical Structure

Molecular Weight: 334.33

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 Pim LSD1 JMJD G9a/GLP MLL NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human THP1 cells	Function assay			Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation, IC50=1.5 μM	18620381
human HepG2 cells	Function assay			Inhibition of ACAT in human HepG2 cells, IC50=0.479 μM	19167888
rat macrophages	Function assay		24 h	Inhibition of ACAT in rat macrophages assessed as incorporation of extracellular [3H]-oleic acid-BSA complex into the intracellular cholesteryl ester after 24 hrs, IC50=0.479 μM	19464189
MCF7	Apoptosis assay	10 uM	6 hrs	Induction of apoptosis in human MCF7 cells assessed as apoptotic cells at 10 uM after 6 hrs by FITC-Annexin V/propidium iodide staining-based FACS analysis relative to control	25801160
MCF7	Apoptosis assay	10 uM	6 hrs	Induction of apoptosis in human MCF7 cells assessed as dead cells at 10 uM after 6 hrs by FITC-Annexin V/propidium iodide staining-based FACS analysis relative to control	25801160
MCF7	Function assay	100 uM	1 hr	Competitive inhibition of DNMT1 in (S)-Methyl 2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-(5-(prop-2-yn-1-yloxy)-1H-indol-3-yl)propanoate labeled human MCF7 cells at 100 uM preincubated for 1 hr followed by cell labeling for 30 mins and clicked with TER-PE	25801160
MCF7	Function assay	50 to 500 uM	1 hr	Competitive inhibition of DNMT1 in (S)-Methyl 2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-3-(5-(prop-2-yn-1-yloxy)-1H-indol-3-yl)propanoate labeled human MCF7 cells at 50 to 500 uM preincubated for 1 hr followed by cell labeling for 1 hr and clicked with TER	25801160
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	334.33	Formula	C₁₉H₁₄N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	48208-26-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N-Phthalyl-L-tryptophan			Smiles	C1=CC=C2C(=C1)C(=O)N(C2=O)C(CC3=CNC4=CC=CC=C43)C(=O)O

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (197.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 66 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.
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.
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.	3.350mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 67 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.
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.	3.350mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 67 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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.415mg/ml (1.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	DNA methyltransferase ^[1] (Cell-free assay) 115 nM
In vitro	RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of this compound results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, it causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences. ^[1] In another study, the synthesis and in vitro analysis of a biotinylated conjugate of this chemical is investigated to evaluate the interactions with DNA methyltransferase enzymes. ^[2] In a recent study, it is shown this compound can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs. ^[3]
Kinase Assay	In vitro methylation assay
Kinase Assay	The substrate DNA for the in vitro methylation assay is a 798 bp fragment (−423/+375 relative to the initiation codon) from the promoter region of the human p16Ink4a gene. The methylation reaction contains 350 to 400 ng substrate DNA and 4 units of M.SssI methylase (0.5 μM) in a final volume of 50 μL. This compound is added to final concentrations of 10, 100, 200, and 500 μM, respectively. Reactions are done at 37 °C for 2 hours. After completion, the reaction is inactivated at 65 °C for 15 minutes and the DNA is purified using PCR Purification kit. Three hundred nanograms of purified DNA is digested for 3 hours at 60 °C with 30 units of BstUI and analyzed on 2% Tris-borate EDTA agarose gels.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16024632/ [2] https://pubmed.ncbi.nlm.nih.gov/16536454/ [3] https://pubmed.ncbi.nlm.nih.gov/21886809/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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