RN-1 (hydrochloride)

RN-1 is a potent, irreversible inhibitor of LSD1 (IC₅₀ = 70 nM).¹ It is much less effective against MAO-A and MAO-B (IC₅₀s = 0.51 and 2.8 µM, respectively).¹ Following intraperitoneal administration, RN-1 penetrates the blood-brain barrier and distributes in mice to a brain/plasma exposure ratio of 88.9.¹ It blocks long-term but not short-term memory in mice.¹ RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.^2,3

WARNING This product is not for human or veterinary use.

1. Neelamegam, R., Ricq, E.L., Malvaez, M., et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. ACS Chem. Neurosci. 3(2), 120-128 (2012).

2. Konovalov, S., and Garcia-Bassets, I. Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines. J. Ovarian Res. 6(1), 75 (2013).

3. Cui, S., Lim, K.C., Shi, L., et al. The LSD1 inhibitor RN-1 induces fetal hemoglobin synthesis and reduces disease pathology in sickle cell mice. Blood 126(3), 286-296 (2015).

Bailey, C.P., Figueroa, M., Gangadharan, A., et al. Scaffolding LSD1 inhibitors impair NK cell metabolism and cytotoxic function through depletion of glutathione. Front. Immunol. 11, 2196 (2020).