CNS-penetrant, selective restorer of injury- or disease-induced overproduction of proinflammatory cytokines towards homeostasis. Selective suppressor of beta amyloid (Aβ)-induced glia proinflammatory cytokine production

Novel potent and selective cathepsin K (Cat K) inhibitor

Novel potent mutant IDH1 R132H inhibitor

Novel potent and selective MCL-1 inhibitor

Novel potent MurA inhibitor

Novel potent multitarget ligand

Useful probe in the mapping of membrane proteins, such as ion channels and transports proteins, as well as enzymes and receptors.

Useful probe in the mapping of membrane proteins, such as ion channels and transports proteins, as well as enzymes and receptors.

Novel mitochondria-targeted photoactivatable real-time probe, being phototriggered by either UV (one-photon) or NIR (two-photon) light to form a fluorescent coumarin product and facilitate the release of drug payload

Novel mTOR inhibitor, exhibiting potent anticancer activities against four tumor cell lines, including MCF-7, HeLa, MGC-803, and C6, inducing cell death via apoptosis by targeting both mTORC1 and mTORC2 within cells and arrests the cell cycle of HeLa at t

Novel selective mTORC1 inhibitor, directly targeting class I glucose transporters

Novel selective inhibitor of mTORC1, yielding potent inhibition of glucose uptake

Novel potent dual inhibitor of mTOR and HDAC1

Novel Mithramycin A (MTM) 2'-oxime (MTMox) conjugate, displaying an 11-fold increase in plasma exposure and improved efficacy in an Ewing sarcoma xenograft

Selective antagonist of melanocortin-4 receptor (MC4R)

Novel resveratrol-based multitarget-directed ligand, cellularly activating the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibiting both hMAO-B and QR2 (IC 50 s = 8.05 and 0.57 μM), and promoting hippocampal neurogenesis

Novel minimized theta-defensin, being highly effective against CRE pathogens K. pneumoniae and E. coli in vivo, significantly enhancing survival by promoting rapid host-mediated bacterial clearance and by modulating pathologic cytokine responses, restorin

Novel antituberculosis agent. targeting the respiratory chain of Mycobacterium tuberculosis (Mtb) and being effective against multi drug resistant (MDR) Mtb

Novel BBB permeable potent MT1 and MT2 ligand (MT1, Ki = 0.031 nM; MT2, Ki = 0.070 nM) with good metabolic stability in human hepatic microsomes

Potent TRPV1 agonist

Novel potent and selective PI3Kδ inhibitor

Novel inhibitor of SLC16A3

Novel potent tankyrase (TNKS) inhibitor (EC 50 : 2 nM)

Mitochondrial tRNA-specific modification, regulating efficient mitochondrial translation and energy metabolism in mammals

Novel potent and selective SETD8 inhibitor

Novel inhibitor of Human p53 and CREB Binding Protein (CREBBP) interaction

Novel inhibitor of DNA damage repair

Inhibitor of DNA damage repair

Novel, selective, orally bioavailable, negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5)

Novel inhibitor of Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor