NS-1643 is an activator of the human ether-a-go-go related gene (ERG1, KCNH2, hERG) KV11.1 channel. NS-1643 shows significantly increase both steady-state and peak tail currents of hERG channels but exhibits only a trivial effect on Kv4.3 and Kv1.5 channels. Causes a significant reduction in action potential duration in patch clamp assays in Xenopus oocytes, HEK293 cells, and guinea pig cardiomyocytes that can be reversed by the addition of E-4031, a specific blocker of hERG channels. Also shown to activate IKr channel in cardiomyocytes and increase post-repolarization refractory time thereby alleviating hyper-excitability and producing antiarrhythmic effects. NS-1643 can also restore IKr reduced by down-regulation of IKr expression. NS-1643 also activates the KV11.2 (ERG2, KCNH6) channel, but evokes a distinctly different response from that of KV11.1. NS-1643 is commonly used for Biochemicals applications.

BAY 41-8543 (2-[1-[(2-fuorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5(4-morpholinyl)-4,6-pyrimidinediamine) is s potent nitric oxide (NO)-independent stimulator of soluble guanylate cyclase (sGC). BAY 41-8543 manifested both antiplatelet effect and vasodilatation. It has the potential of being a unique clinical utility for the treatment of cardiovascular diseases.

Levovirin is a guanosine nucleoside analog and the L-enantiomer of ribavirin. It is an investigational drug for the treatment of hepatitis C virus-mediated diseases. Levovirin has a similar immunomodulatory potency to ribavirin in vitro without accumulating in red blood cells or causing hemolytic anemia, a known side effect of ribavirin. Levovirin has been shown to stimulate host immune responses (enhanced Th1 and reduced Th2 cytokine expression). Significantly improved oral absorption of levovirin was achieved following administration of a valine ester prodrug of levovirin R1518. Levovirin was found more potent to inhibit Tick-borne encephalitis virus (TBEV) on the basis of robust binding affinity between protein-drug interactions. This finding may help to understand the nature of helicase and development of specific anti-TBEV therapies.

Notoginsenoside R1 is a characteristic constituent of Radix notoginseng, a well known herbal medicine widely used in Asian countries for treating microcirculatory disturbance-related diseases, such as diabetic nephropathy, cardiovascular disease, cerebral vascular disease, and liver dysfunction. Notoginsenoside R1 has multiple pharmacologic activities, including cardioprotective, neuroprotective, anti-inflammatory, and anticancer effects. A study on the application of Notoginsenoside R1 in a rat model of diabetic nephropathy indicated that Notoginsenoside R1 ameliorated the glucose-induced impairment of podocyte adhesive capacity and subsequent podocyte depopulation, partly through the upregulation of α3β1 integrin via PI3K-Akt signaling pathway activation.

Citrinin is a mycotoxin produced by several species of the genera Aspergillus, Penicillium and Monascus. It is often found in food. Citrinin is nephrotoxic agent. Inhibition of RNA (predominantly rRNA) and DNA synthesis by citrinin has been reported in different mammalian cell lines including kidney cells. The induction of oxidative stress has also been proposed to account for citrinin toxicity. Citrinin inhibits immune response – it inhibits lipopolysaccharide/interferon-gamma-induced nitric oxide production in glomerular mesangial cells. Citrinin induced apoptosis in human colon cancer and promyelocytic leukemia cell lines.

Tomatidine is a steroidal alkaloid derived from green tomato. Tomatitidine has been identified as a potential therapeutic agent or lead compound for the treatment of skeletal muscle atrophy. It has been shown to increase skeletal muscle mTORC1 signaling, reduce skeletal muscle atrophy, enhance recovery from skeletal muscle atrophy, stimulate skeletal muscle hypertrophy, and increase strength and exercise capacity. In addition, tomatidine has been identified as a potential therapeutic agent or lead compound for reducing the activity of Activating Transcription Factor 4 (ATF4).

Verrucarin A (VC-A) is a Type D macrocyclic mycotoxin which inhibits cell proliferation and induces apoptosis in cancer cells. Strong antiproliferative and apoptosis-inducing activity of verrucarin A for pancreatic ductal adenocarcinoma and prostate cancer cells through cell cycle arrest and inhibition of the prosurvival (antiapoptotic) AKT/NF-κB/mTOR signaling.has being demonstrated. Verrucarin A, a protein synthesis inhibitor, also induces growth inhibition and apoptosis in breast cancer cell lines MDA-MB-231 and T47D.

Sophoridine is a quinolizidine alkaloid isolated from traditional Chinese herbs, which exists in the stems and leafs of Leguminous plant Sophora alopecuroides L., Euchresta japonica Benth., and the roots of Sophora alopecuroides Ait. Sophoridine-induced synchronous oscillations in the hippocampus could elicit the generation and development of seizure. Accumulating evidence demonstrates remarkable pharmacological effects of Sophoridine, including anti-inflammatory, anti-virus and anti-cancer effects. Sophoridine is promising to be a novel, potent and selective antitumor drug candidate for pancreatic cancer. It was shown that sophoridine is able to suppress hepatocellular carcinoma in vitro and vivo. Sophoridine dose- and time-dependently blocks the RANKL-induced osteoclasts formation and the activation of ERK and c-Fos as well as the induction and nucleus translocation of NFATc1.

Isoorientin is a common C-glycosyl flavone in the human diet. It has been isolated from several plant species, including Phyllostachys pubescens, Crataegus monogyna and Crataegus pentagyna, Patrinia villosa Juss, Drosophyllum lusitanicum, buckwheat, Arum palaestinum, and Rumex and Swertia. Isoorientin possesses significant anti-nociceptive and anti-inflammatory activities. Significantly protected PC12 nerve cells from 6-OHDA-induced apoptotic neurotoxicity and reduced the proliferation of HepG2 cells. Isoorientin showed anti-RSV (respiratory syncytial virus) activity.