[1527503-11-2]    

MFCD28133403

Synonyms : 5'-Methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine

Applications : A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.

References : Reiner D. et al. Sci Rep., 10(1), 13558, 2020; Wagner T. et al.: Nucleic Acids Res., 44(9), e88, 2016; Sweis R. F. et al.: ACS Med Chem Lett., 5(2), 205-209, 2014; Pappano W. N. et al.: PLoS One 10(7), e0131716, 2015.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.