RG108 48208-26-0

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Molecular Weight: 334.33 RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM, does not cause trapping of covalent enzymes.


Biological Activity


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 RG108 results in significant
demethylation of genomic DNA without any detectable toxicity.
Intriguingly, RG108 causes demethylation and reactivation of tumor
suppressor genes, but it does not affect the methylation of centromeric
satellite sequences. In another study, the synthesis and in vitro
analysis of a biotinylated RG108 conjugate is investigated to evaluate
the interactions with DNA methyltransferase enzymes. In a recent study,
it is shown RG108 can significantly reduce the DNA methyltransferases
activity in SM derived iPS cells as compared to the native SMs.


Protocol(Only for Reference)


Kinase Assay: [1]

In vitro methylation 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. Inhibitors are 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.

Cell Assay: [1]

Cell lines	HCT116 cells
Concentrations	1-100 μM
Incubation Time	5 days
Method	For the determination of cellular growth and viability, cells are stained with trypan blue and counted using a standard counting grid.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	334.33
Formula	C19H14N2O4
CAS No.	48208-26-0

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	67 mg/mL (200.4 mM)
		Water	<1 mg/mL (
		Ethanol	67 mg/mL (200.4 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	1H-Indole-3-propanoic acid, α-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-, (αS)-

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Product Categories : Epigenetics > DNA Methyltransferase Inhibitor