NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response.
NFAT inhibitor. Inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). Also attenuates NO production and Nos2 mRNA expression in LPS-stimulated BMDMs. Improves symptoms in a mouse
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer’s disease (AD) and aging-related disorders research[1]. Q134R (1-10 μM) suppresses NFAT signaling, without inhibiting calcineurin activity. Q134R partially inhibits NFAT activity in primary rat astrocytes, but does not prevent calcineurin-mediated dephosphorylation of a non-NFAT target, either in vivo, or in vitro[1]. Q134R (4 mg kg; orally gavage; twice per day; for 7 days) treatment improves cognitive function in rodent models of AD‐like pathology[1]. [1]. Pradoldej Sompol, et al. Q134R: Small chemical compound with NFAT inhibitory properties improves behavioral performance and synapse function in mouse models of amyloid pathology. Aging Cell. 2021 Jul;20(7):e13416.