Fluorescein isothiocyanate (FITC) is widely used to attach a fluorescent label to proteins via the amine group. The isothiocyanate group reacts with amino terminal and primary amines in proteins. It has been used for the labeling of proteins including antibodies and lectins. Isomer I (Fluorescein 5-isothiocyanate) has the thiocyanate group on the 4 carbon of the benzene ring, whereas isomer II (Fluorescein 6-isothiocyanate) has the thiocyanate on the 5 carbon. The two isomers are indistinguishable spectrally, either by wavelength or intensity. Isomer I is more easily isolated in pure form, so is less expensive. This may explain why isomer I is more commonly used for labeling. For many purposes, however, the mixed isomers of FITC will be perfectly suitable. Some FITC conjugates are being investigated for diagnostic purposes. Folate-fluorescein isothiocyanate, or folate-FITC, also identified as EC-17, targets folate receptors over expressed in certain cancers and could help in better identifying the margins of the cancer thereby achieving negative margins.

INCB3284 or INCB-3284 Incyte’s internally developed, oral human CCR2 antagonist for the treatment of chronic inflammations. It is in Phase IIa trial of patients with rheumatoid arthritis (RA).

SB-743921 is a synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits the ATP-binding domain of the kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis. SB-743921 has greater than 40,000 fold selectivity for KSP over other kinesins. SB-743921 has demonstrated promising anti-cancer activity in a variety of in vivo and in vitro human cancer models in preclinical studies. Furthermore, anti-cancer effect has been demonstrated in taxane-refractory malignancies with SB-743921. Toxicity studies demonstrated predictable neutropenias and gastrointestinal toxicities without clear evidence of neurotoxicity. The recommended phase II dose for SB-743921 as a 1-h infusion every 21 days is 4 mg/m2.

D-Galacturonic acid is the main constituent of pectin, a naturally abundant compound. It is the monobasic acid resulting from oxidation of the primary alcohol group of D-galactose to carboxyl. D-Galacturonic acid prepared from pectin can be used to synthesize vitamin C. Native pectin is a mixture of polysaccharides, with the major component a polymer of -D-galacturonic acid. Pectin has numerous other medical and pharmaceutical uses, for example in combination with plant hemicelluloses and lignin, may be useful dietary constituents in preventing coronary heart disease, diverticular disease, ulcerative colitis, and a variety of other Western diseases. Pectin, a representative diety fibre, is a gelatinous substance derived from the cell walls of fruits and some plants and contains galacturonan, consisting of mostly long-chain D-galacturonic acids combined into units by α-1,4 linkages. As a kind of soluble dietary fiber, pectin has been proved of controlling glucose and blood lipids. It slows rapid infusion of the liquid meal into the gut by delaying gastric emptying.

Picolinic acid is an organic compound, is a derivative of pyridine with a carboxylic acid substituent at the 2-position. Picolinic acid is a bidentate chelating agent of elements such as chromium, zinc, manganese, copper, iron, and molybdenum in the human body. Many of its complexes are charge-neutral and thus lipophilic. After its role in absorption was discovered, zinc dipicolinate dietary supplements became popular as they were shown to be an effective means of introducing zinc into the body. Picolinic Acid is an endogenous metabolite of L-tryptophan (TRP) that has been reported to possess a wide range of neuroprotective, immunological, and anti-proliferative effects within the body. However, the salient physiological function of this molecule is yet to be established. The synthesis of picolinic acid as a product of the kynurenine pathway (KP) suggests that, similar to other KP metabolites, picolinic acid may play a role in the pathogenesis of inflammatory disorders within the CNS and possibly other organs.

4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862) is an 1-arylpyrazole class of sigma-1 receptor antagonist. Formalin-induced nociception (both phases), capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity were dose-dependently inhibited by systemic administration of S1RA. Occupancy of sigma-1 receptors in the CNS was significantly correlated with the antinociceptive effects. As a mechanistic correlate, electrophysiological recordings demonstrated that pharmacological antagonism of sigma-1 receptors attenuated the wind-up responses in spinal cords sensitized by repetitive nociceptive stimulation. Esteve is developing E 52862 for the treatment of several pain indications, including diabetic neuropathies, chemotherapy-induced neuropathic pain, postherpetic neuralgia, postoperative pain. Phase II development of this first-in-class agent is underway in Romania, Spain and Greece.

WIN 55212-2 is the synthetic cannabimimetic compound. It is a potent aminoalkylindole cannabinoid receptor agonist. WIN 55,212-2 increases expression of anti-oxidant Cu/Zn SOD and is able to prevent inflammation induced by Aβ1-42 in cultured astrocytes. It exerts neuroprotective and anti-inflammatory actions against Aβ damage through both CB₁ and CB₂ receptors. WIN 55212-2 attenuates hyperalgesia and allodynia in a rat model of neuropathic pain. In the clinical trial, it was revealed that WIN 55212-2, applied topically, decreases the intraocular pressure of human glaucoma resistant to conventional therapies within the first 30 min.

S-fluoxetine is an enantiomer of fluoxetine, a potent and selective inhibitor of the neuronal serotonin-uptake carrier and a clinically effective antidepressant. R-fluoxetine and S-fluoxetine enantiomers are nearly equipotent at blocking serotonin reuptake. In all biochemical and pharmacological studies, the eudismic ratio for the fluoxetine enantiomers is also near unity. A study examining the relative contributions of CYP enzymes to the metabolism of S-fluoxetine, and R-fluoxetine found dramatic differences. These data led to discovery programs between Lilly and Sepracor for the individual enantiomers. S-fluoxetine was studied in a phase 2 clinical trial for the prophylaxis of migraine, however, development was discontinued.

JTE-607 is a multiple cytokine inhibitor. JTE-607 inhibited inflammatory cytokine production, including tumour necrosis factor (TNF)-alpha, interleukin IL-1beta, IL-6, IL-8, and IL-10, from LPS-stimulated human PBMCs. This compound may be useful for the treatment of various cytokine-mediated diseases such as septic shock without causing immunosuppression. JTE-607 may thus be efficacious in cytokine-mediated lung inflammation such as acute respiratory distress syndrome. JTE-607 inhibits the production of IL-10, IL-1ra and C-reactive protein in a human model of endotoxemia. In a leukaemia model engrafted with U-937 cells, JTE-607 significantly prolonged survival in mice and reduced human cytokine mRNA levels in the bone marrow. These results suggest the usefulness of JTE-607 in therapeutic applications for patients with hypercytokinemia and aggressive acute myelogenous leukaemia cell proliferation. JTE-607 had been in phase II clinical trials for the treatment of systemic inflammatory response syndrome but this study was discontinued.

JTC 801 was developed by Japan Tobacco as a novel opioid receptor-like1 (ORL(1)) receptor antagonist. It was found, that JTC-801 completely antagonized the suppression of nociceptin on the forskolin-induced accumulation of cyclic AMP using ORL(1) receptor expressing HeLa cells in vitro. JTC 801 produced analgesic effects and was studied in phase II of a clinical trial for the treatment of neuropathic, cancer and postoperative pain. Nevertheless, that studies were discontinued.