AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg kg QD is well tolerated and results in near stasis (92% TGI) in an HCT116 mouse xenograft model.
LIT-001 free base improves social interaction in a mouse model of autism. LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM).
RP-001 is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
RP-001 hydrochloride is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
BMX-001 is a third-generation, cationic, lipophilic, manganese (Mn), and porphyrin-based mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD). It also has antioxidant and potential chemoprotective activities.