Annonacin is a potent and lipophilic acetogenin from A. muricata that inhibits mitochondrial complex I (IC50 = 54.8 nM).1,2 Annonacin induces ATP depletion, tau pathologies, and dopaminergic cell death in rats (EC50s = 134, 44.1, and 60.8 nM, respectively

The first selective antagonist of orphan receptor GPR18

Novel inhibitor of BAF transcriptional repression

The novel fluorescent probe, allowing lipid droplets and lysosomes to be labelled simultaneously and with high specificity, being visualized readily through yellow and red fluorescence, using different excitation and detection channels

Heat shock protein inhibitor, preventing the synthesis of inducible Hsps, such as Hsp105, Hsp72, and Hsp40, reducing thermotolerance of tumors in SCC VII tumor-containing mice

Novel activator of SIRT1, inducing autophagic cell death via the AMPK-mTOR-ULK complex and inducing mitophagy by the SIRT1-PINK1-Parkin pathway, downregulating 14-3-3γ, catalase, profilin-1, and HSP90α

Naturally occurring inhibitor of FOXO1a nuclear export

Novel and potent EZH2 inhibitor

Potent histamine H3 receptor antagonist

An orally bioavailable, highly potent and selective pan-class I phosphatidylinositol-3 kinase (PI3K) inhibitor

Novel selective PPARγ modulator (sPPARγM), potently inhibiting CDK5-mediated PPARγ phosphorylation and displaying a selective gene expression profile in epididymal WAT

Novel irreversible transglutaminase 2 (TG2) inhibitor

Novel potent and selective inhibitor of mitochondrial respiration supported by pyruvate

Marine cyanobacterium-derived natural antimalarial agent; Potent Inhibitor of the Food Vacuole Falcipains

An isomeric anlog of G140 (AOB13353), acting as an inhibitor of h-cGAS (IC 50 = 0.0428µM)

Novel clickable, electrophilic diazene probe, enabling capture and site-centric proteomic analysis of oxidative post-translational modification (OxiPTM)

Novel agonist of STING (stimulator of interferon genes) with enhanced binding to STING and cellular function

H1-histamine receptor blocker, antiarrhythmic

Novel second-generation SIK inhibitor, inducing not only synthesis of melanin but also melanosomal maturation, export, and localization features, even after import into keratinocytes

Novel inhibitor of ER-to-cytosol protein dislocation, exhibiting anti-dengue and anti-Zika virus activity

The first small molecule modulator of cold inducible RNA-binding protein (CIRBP) activity

The first small molecule modulator of cold inducible RNA-binding protein (CIRBP) activity

Novel potent and selective SMS2 inhibitor, showing more than 1400-fold selectivity over SMS1

Novel immune checkpoint VISTA (V-domain immunoglobulin suppressor of T-cell activation) modulator

Potent and selective inhibitor of Galactokinase (GALK)

Highly potent κ agonist

A novel potent and selective negative modulator of AMPA receptors containing TARP-gamma8

Novel selective GPR120 agonist

Novel neuroprotective agent, significantly reducing Aβ toxicity by delaying paralysis and improving cognitive performances in a transgenic mouse model of AD

Novel activator of SIRT6 deacetylation