Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM. Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM). Kushenol K also inhibits the activity of SGLT1 and SGLT2.

N-(Hydroxymethyl)nicotinamide is an antimicrobic agent.

Rotundifuran, a labdane type diterpene, is isolated from Vitex rotundifolia. Rotundifuran can inhibit the cell cycle progression and induce apoptosis in human myeloid leukaemia cells.

Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests.

Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.

OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.

Maresin 1, produced by human Mφs from endogenous docosahexaenoic acid (DHA) and a specialized proresolving mediator, stimulates intracellular [Ca2+] and secretion. Maresin 1 possesses anti-inflammatory activity.

JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint.

JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint.

AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.

AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.

Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 μM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 μM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 μM).

Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.

Omaciclovir (H2G) is a potent and selective inhibitor of herpesvirus replication. Omaciclovir is a nucleoside analog with antiviral activity.

(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.

Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.

3-Methyl-GABA is an activator of GABA aminotransferase with anticonvulsant activity.

2-Undecanol (Undecan-2-ol) is a male specific volatile identified from the sap beetle Lobiopa insularis. 2-undecanol is a flower emitted volatile, used by various species of Hymenoptera as a pheromone component.

ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.

Bisdionin C is a potent GH18 chitinases inhibitor, with an IC50 of 0.2 μM for A. fumigatus ChiB1 (AfChiB1). Bisdionin C inhibits HCHT (human macrophage chitotriosidase) and acidic mammalian chitinase (AMCase) with IC50s of 8.3 and 3.4 μM, respectively.

VU0420373 is a potent heme sensor system (HssRS) activator with an EC50 of 10.7 μM and a pEC50 of 4.97. VU0420373 induces heme biosynthesis, and is toxic to fermenting S. aureus.

N-Heptanoyl-L-homoserine lactone is a member of N-acyl-homoserine lactone family. N-acyl-homoserine lactones (AHL) regulate gene expression in gram-negative bacteria, such as Echerichia and Salmonella, and are involved in quorum sensing, cell to cell communication among bacteria.

Vanillic acid glucoside is isolated from the fruits of C. annuum as well as the leaves of various additional plants. Vanillic acid glucoside belongs to a class of compounds known as hydrolyzable tannins and can be phytotoxic against different species.

Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.

Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.

Ganglioside GM3 sodium salt is a sialylated membrane-based glycosphingolipid that regulates insulin receptor signaling via direct association with the receptor. Ganglioside GM3 sodium salt possesses powerful effects on cancer development and progression.

STING ligand-1 is a lead STING ligand with an IC50 of 68 nM for HAQ STING.

PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.