A 366

Name: A 366
Brand: Tocris Bioscience
SKU: 5163

Tocris Bioscience, part of Bio-Techne | Catalog # 5163

Citations (4)

COA / SDS

Potent and selective G9a/GLP inhibitor

Key Product Details

Description:	Potent and selective G9a/GLP inhibitor
Chemical Name:	5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
Purity:	≥98% (HPLC)
Molecular Weight:	329.44

View Full Technical Details for A 366

Technical Data
Citations

Biological Activity for A 366

A 366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC₅₀ = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A 366 probe summary on the SGC website.

Compound Libraries for A 366

A 366 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 366 is reviewed on the chemical probes website.

Technical Data for A 366

M. Wt	329.44
Formula	C₁₉H₂₇N₃O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1527503-11-2
PubChem ID	76285486
InChi Key	BKCDJTRMYWSXMC-UHFFFAOYSA-N
Smiles	COC1=C(OCCCN4CCCC4)C=C(N=C(N)C32CCC3)C2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for A 366

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	1eq. HCl	32.94	100
	DMSO	32.94	100

Preparing Stock Solutions for A 366

The following data is based on the product molecular weight 329.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.04 mL	15.18 mL	30.35 mL
5 mM	0.61 mL	3.04 mL	6.07 mL
10 mM	0.30 mL	1.52 mL	3.04 mL
50 mM	0.06 mL	0.30 mL	0.61 mL

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References for A 366

References are publications that support the biological activity of the product.

Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
Sweis Discovery and development of potent and selective inhibitors of histone methyltransferase G9a. ACS Med.Chem.Lett. 2014 PMID: 24900801