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Histone Methytransferase

A-366 (1527503-11-2)

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC₅₀ = 3.3 nM). It displays >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. A-366 has been shown to inhibit H3K9 methylation in prostate cancer PC3 cells with an IC₅₀ of 100 nM.

Not Intended for Therapeutic Use. For research use only.

CAS: 1527503-11-2 Category

A-366 (1527503-11-2) Description

A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM). It displays greater than 1,000-fold selectivity over 21 other methyltransferases. A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2. It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).


A-366 (1527503-11-2) Specifications

Product Name A-366
Synonyms A 366; A366.
Chemical Name 5′-methoxy-6′-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3′-indole]-2′-amine
Drug Class Inhibitor
Purity >98%
CAS Number 1527503-11-2
Molecular Formula C19H27N3O2
Molecular Weight 329.444 g/mol
Monoisotopic Mass 329.21 g/mol
MDL number MFCD28133403
InChi Code InChI=1S/C19H27N3O2/c1-23-16-12-14-15(21-18(20)19(14)6-4-7-19)13-17(16)24-11-5-10-22-8-2-3-9-22/h12-13H,2-11H2,1H3,(H2,20,21)
Form Powder
Color white to beige
Solubility  DMSO: 10 mg/mL
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >3 years if stored properly
Handling Protect from air and light
Application G9a/GLP inhibitor


RIDADR NONH for all modes of transport


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