Arundic Acidis is an astrocyte modulating agent, in acute ischemic stroke. It is a therapeutic agent for the treatment of neurodegenerative diseases including Alzheimer’s disease and Parkinson’s disease.

AR-9281 is a soluble epoxide hydrolase (s-EH) inhibitor potentially for the treatment of hypertension and type 2 diabetes.

Anecortave Acetate is an angiostatic steroid used for proteomics research.

AM-2233 is a highly potent full agonist for the cannabinoid receptors. It was developed as a selective radioligand for the cannabinoid receptors and has been used as its 131I derivative for mapping the distribution of the CB1 receptor in the brain. AM-2233 was found to fully substitute for THC in rats, with a potency lower than that of JWH-018 but higher than WIN 55,212-2.

AM-1248 is a drug that acts as a moderately potent agonist for both the cannabinoid receptors CB1 and CB2.

AM-1235 is a drug that acts as a potent and is selective agonist for the cannabinoid receptor CB1.

AM 114 is a proteasome inhibitor. It is an inhibitor of chymotrypsin-like activity of the 20S proteasome. Also, AM-114 displays anticancer activity, inhibits cell growth in human colon cancer HCT116 p53+/+ cells.

Alatrofloxacin Mesylate is the parental prodrug of Trovafloxacin, a broad-spectrum antibiotic.

Abafungin is a broad-spectrum antifungal agent.

MSC 2032964A is a potent and selective ASK1 inhibitor (IC50 = 93 nM). It blocks LPS-induced ASK1 and p38 phosphorylation in cultured mouse astrocytes and suppresses neuroinflammation in a mouse EAE model. MSC 2032964A is orally bioavailable and brain penetrant.

Aphidicolin is a tetracyclic diterpene antibiotic isolated from the fungus, Cephalosporum aphidicola with antiviral and antimitotic properties. Aphidicolin is a reversible inhibitor of eukaryotic nuclear DNA replication. It blocks the cell cycle at early S phase. It is a specific inhibitor of DNA polymerase A,D in eukaryotic cells and in some viruses (vaccinia and herpesviruses) and an apoptosis inducer in HeLa cells. Natural aphidicolin is a secondary metabolite of the fungus Nigrospora oryzae.

Prostratin is a protein kinase C activator found in the bark of the mamala tree of Samoa, Homalanthus nutans (Euphorbiaceae). While prostratin was originally isolated and identified as a new phorbol from species of the genus Pimelea (Thymelaceae) in Australia, the antiviral activity of prostratin was discovered during research on the traditional knowledge of Samoan healers in Falealupo village by ethnobotanist Paul Alan Cox and a team at the U.S. National Cancer Institute. Samoan healers use the mamala tree to treat hepatitis. Research indicated that prostratin has potential to be useful in the treatment of HIV as it could flush viral reservoirs in latently infected CD4+ T-cells. As a modulator of Protein Kinase C, it has been shown to exhibit promising therapeutic potential against other diseases such as cancer and Alzheimer's disease. In 2015, study showed that orally administrated prostratin repressed human pancreatic tumor. (Source: https://en.wikipedia.org/wiki/Prostratin). (Last update: 4/1/2016).

MI-192 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC2 (IC50 = 30 nM) and HDAC3 (IC50 = 16 nM) over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively).

2-Phospho-L-ascorbic acid trisodium salt is a stable ascorbic acid derivative used in cell culture. In combination with FGF-2, it maintains differentiation potential in bone marrow-derived mesenchymal stem cells (MSC) through increased expression of HGF. L-Ascorbic acid 2-phosphate may be used in cell differentiation and tissue engineering applications. 2-Phospho-L-ascorbic acid trisodium salt also exhibits synergistic protection of hMSCs under oxidative stress in combination with N-acetylcysteine. Asc-2P is used in studies of gene repression, such as the repression of dihydrotestosterone-induced dickkopf-1 expression. AA2P has been shown to increase myogenin gene expression and promote differentiation in L6 muscle cells.

Tilfrinib is a potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 3.15 nM). Tilfrinib has >1000-fold selectivity for Brk over a panel of other kinases and inhibits proliferation of breast cancer cells in vitro.

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.

Gly-Pro-Glu, also known as GPE, is a neuroprotective agent and the N-terminal tripeptide of IGF-1. Gly-Pro-Glu is neuroprotective after central administration in animal models of neurodegenerative processes, such as Huntington’s, Parkinson’s, Alzheimer’s diseases, and varies acute brain injury animal models. GPE mimics insulin-like growth factor I effects on the somatostatin system through a mechanism independent of β-amyloid clearance that involves modulation of calcium and glycogen synthase kinase 3β signaling.

SQ109 is a drug undergoing development for treatment of tuberculosis. SQ109 showed activity against both drug susceptible and Multi-drug-resistant tuberculosis bacteria, including Extensively drug-resistant tuberculosis strains. In preclinical studies SQ109 enhanced the activity of anti-tubercular drugs isoniazid and rifampin and reduced by >30% the time required to cure mice of experimental TB. SQ109 is being developed by OOO Infectex in Russia and by Sequella Inc internationally. I

Y-29794 Tosylate is an orally active, potent and specific non-peptide prolyl endopeptidase (PPCE) inhibitor. Y-29794 selectively and competitively inhibited rat brain PPCE (Ki = 0.95 nM) in a reversible manner. Ex vivo study demonstrated that Y-29794 could penetrate into brain to exhibit dose-dependent and long-lasting inhibition. Furthermore, Y-29794 could potentiate the effect of TRH on the release of ACh in the rat hippocampus. Y-29794 prevents the progression of A beta-like deposition in the hippocampus of the SAM.

MK-7622 is a cholinesterase inhibitor under evaluation for the treatment of Alzheimer's disease. No studies have been published on this compound in the peer-reviewed literature or other publicly available documents. In October 2013, Merck began a Phase 2 trial in the United States to evaluate the compound's tolerability and efficacy as a symptomatic adjunct to donepezil therapy in patients with probable AD as diagnosed by two conventional diagnostic criteria, the NINCDS-ADRDA and DSM-IV.

UNIL088 is a water-soluble prodrug of cyclosporine A (CsA) designed for topical ocular delivery. The pro-moiety is grafted via an ester function to CsA and the solubilizing group is a phosphate ion. UNIL-088 can be rapidly hydrolysed under physiological conditions, and can retain a long shelf-life in aqueous media. UNIL-088 is more stable at pH 5 than at pH 7 with conversion rate constant of 3.2 x 10(-3) and 26.0 x 10(-3)days(-1), respectively.

ML192, also known as MLS000526305 and CID1434953, is a selective ligands for GPR55. The orphan G protein coupled receptor, ML192 (CID1434953) with 1080 nM potency for GPR55 and >45-fold antagonist and agonist selectivity against GPR35, CB1 and CB2. GPR55 has gained notoriety because of its putative identification as a cannabinoid receptor subtype. The significance of this assignment should not be underestimated given the importance of cannabinoids to drug abuse and the potential utility of cannabinoid ligands in treating behavioral disorders leading to conditions such as obesity.

GSK-7975A is an potent and orally active inhibitors of ORAI1 (calcium release-activated calcium modulator ). GSK-7975A prevents Cytosolic Calcium-Associated Injury of Human Pancreatic Acinar Cells and Acute Pancreatitis in 3 Mouse Models. GSK-7975A inhibited toxin-induced activation of ORAI1 and/or activation of Ca(2+) currents after Ca(2+) release, in a concentration-dependent manner, in mouse and human pancreatic acinar cells (inhibition >90% of the levels observed in control cells). ORAI1 inhibitors might be developed for the treatment of patients with pancreatitis.

ST247 is a PPAR β/δ selective inverse agonist. ST247 IC50 = 19 nm vs. GSK0660 IC50 = 210 nM.

UBP-310 is a potent and selective GLUK5 kainate receptor antagonist (IC50 = 130 nM). UBP-310also blocks recombinant homomeric GLUK7 receptors.

PF-04937319 is a glucokinase activator which is under development for the treatment of type 2 diametes mellitus. Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primarily through its regulatory actions in pancreatic β-cells and liver hepatocytes. Conversion of glucose to glucose-6-phosphate by GK promotes glycogen synthesis in liver hepatocytes, and insulin release in the pancreatic β-cells.

OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism.

XMD8-85, also known as ERK5-IN-1, exhibits potent inhibition of ERK5 and LRRK2.

PF-06442609 is a potent, metabolic stable γ-secretase modulators (GSMs) for Alzheimer's disease (AD). PF-06442609 displayed a favorable rodent pharmacokinetic profile, and robust reductions of brain Aβ42 and Aβ40 were observed in a guinea pig time-course experiment. F-06442609 is suitable for rodent model of AD.

VU0483605 is a potent and selective positive allosteric modulator (PAM) of mGluR1, displaying EC50 values of 0.39 and 0.36 μM at human and rat receptors, respectively, and no activity as a mGlu4 PAM (EC50 >10 μM).