Neotetrazolium chloride is used for the histochemical detection of dehydrogenases. Neotetrazolium reduction can be used for discriminating malignant cells from nonmalignant cells. Neotetrazolium chloride is used for the colorimetric estimation of succinic dehydrogenase activity in a tumor sensitivity test to chemotherapeutic agents. Neotetrazolium chloride is also used in the microagglutination test and in the Neotetrazolium Test (NTC) for histologic evaluation of myocardial sections in acute necrobiosis of the myocardium.

Cytochalasin D, a tropical fungal metabolite, is a disruptor of actin filament function, resulting in multinucleated cell formation, reversible inhibition of cell movement, and the induction of cellular extrusion. It was shown that cytochalasin D inhibits murine CT26 colorectal carcinoma cells growth and angiogenesis.

L-MTX is a second-generation tau protein aggregation inhibitor. It acts by reducing levels of aggregated or misfolded tau proteins, which are associated with the progressive neurodegeneration. It is currently under development for the treatment of Alzheimer’s disease.

Procaspase-activating compound 1, PAC-1, has been introduced as a direct activator of procaspase-3 and has been suggested as a therapeutic agent against cancer. Its activation of procaspase-3 is dependent on the chelation of zinc. In 2015, a phase I clinical trial of PAC-1 opened for enrollment of cancer patients, and in 2016, it was announced that PAC-1 had been granted Orphan Drug Designation for treatment of glioblastoma by the FDA.

FENPYROXIMATE is a pyrazole acaricide widely used in the prevention of acarids (mites) in fruit plant gardens. It is a potent inhibitor of the mitochondrial proton-translocating NADH-quinone oxidoreductase (complex I).

Toluidine Blue (also known as tolonium chloride or Toluidine blue O) is metachromatic dye used for a variety of histological staining, it selectively stains acidic tissue components (sulfates, carboxylates, and phosphate radicals. Toluidine blue has an affinity for nucleic acids, and therefore binds to nuclear material of tissues with a high DNA and RNA content. It was evaluated the toluidine blue staining in premalignancies, and superficial oral ulceration suggesting malignancy. The study showed 100% sensitivity in the detection of in situ and invasive carcinoma and no false-negative results occurred. The lesions that were diagnosed as dysplasia did not retain stain, and thus gave false-negative results. The reasons could be that the exact mechanisms by which the dye differentially stains malignant or dysplastic tissues remain unknown.

Birinapant is a parenterally administered bivalent peptidomimetic of the SMAC protein (Second Mitochondria-derived Activator of Caspases) and is therefore known as a SMAC mimetic compound. Birinapant is a particularly potent antagonist of two members of the Inhibitor of Apoptosis Proteins (IAP) family, cIAP-1, and cIAP-2. cIAP-1 and -2 are ubiquitin ligases whose expression can protect cells from apoptosis and cause pro-survival effects of TNF-α and related ligands. When Birinapant binds to cIAP-1 or -2 it causes the protein to ubiquitinate itself, which in turn drives the degradation of the protein. In this way, birinapant suppresses the levels of cIAP-1 and cIAP-2 and therefore switches cell signaling to drive tumor cell apoptosis in the presence of TNF-α. Birinapant has been shown to give rise to sustained and substantial reductions of cIAP1 levels in Peripheral Blood Mononuclear Cells (PBMCs) and tumor tissue. To date, Birinapant has been dosed in approximately 450 patients across 9 studies. The majority of studies was in oncology (one in HBV) and primarily recruited patients with refractory solid tumors & hematological malignancies (dominated by ovarian, colorectal, acute myeloid leukemia and Myelodysplastic syndromes). Overall Birinapant has shown acceptable safety and tolerability for further development in oncology indications. The current plans are to study Birinapant clinically in combination with Keytruda® for the treatment solid tumors and in an Investigator-Initiated study at UCLA for high-grade serous carcinoma (HGSC) in combination with platinum-based chemotherapy.

Azaspirium was studied as a spasmolytic and antihypertensive agent.