Anaxirone is a synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis. This agent has been shown to exhibit a broad spectrum of antineoplastic activity against experimental tumors, including those resistant to other alkylating agents.

EP6 is a 5-lipoxygenase (5-LO) inhibitor. 5-LO is a crucial enzyme of the arachidonic acid (AA) cascade and catalyzes the formation of bioactive leukotrienes (LTs) which are involved in inflammatory diseases and allergic reactions.

Aroplatin is a synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotoxicity. Because DNA mismatch-repair (MMR) complexes do not recognize DACH–platinum adducts, DNA repair mechanisms are inhibited, overcoming limitations observed with other platinum-based agents. In addition, the liposomal encapsulation improves the bioavailability of NDDP and reduces its toxicity profile.

Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor drug candidate. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of streptozotocin (STZ)-induced diabetes. Cenupatide was found to revert STZ-induced up-regulation of uPA levels and activity, while uPAR on podocytes and (s)uPAR were unaffected. In glomeruli, Cenupatide inhibited FPR2 expression suggesting that the drug may act downstream uPAR, and recovered the increased activity of the αvβ3 integrin/Rac-1 pathway indicating a major role of uPAR in regulating podocyte function.

Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis.ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro. ITF2357 decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro.

KG-5 is an orally available PDGFRß and B-Raf allosteric inhibitor.

Hexamide is a protein inhibitor.

AT9283 is a multikinase inhibitor, is also a small-molecule inhibitor of several kinases with potential antineoplastic activity. Multikinase inhibitor AT9283 binds to and inhibits Aurora kinases A and B, JAK2 (Janus kinase 2) and the kinase BCR-ABL, which may result in the inhibition of cellular division and proliferation and the induction of apoptosis in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis; JAK2 is a kinase that transduces signals from the single chain and IL-3 cytokine receptor families, and from the IFN-gamma receptors; BCR-ABL is a fusion protein with tyrosine kinase activity that is commonly found in CML.

Exatecan, also known as DX 8951, is a semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues.

Simetride is used in the Reversal of resistance to vincristine in P388 leukemia. Simetride is a non-narcotic analgesic, it is an ingredient of Kyorin AP2 (a combination of Simetride and Anhydrous Caffeine (40:1)) in Japan. Kyorin AP2 is used to treat low back pain, symptomatic neuralgia, headache, menstrual pain, pharyngalgia/earache due to inflammation, toothache, postoperative pain.

Apadoline, also known as RP 60180, is a non-peptidic kappa-opioid receptor agonist. From the dose of 1 mg/kg i.v., RP 60180 slowed ECG frequency. This effect, which lasted for about 30 minutes post-injection, was most often seen at the higher doses. According to literature, both RP 60180 and pentazocine reduced pain-related CSSERP amplitudes by approximately 40%. Pentazocine tended to produce more side effects.

Bemitradine is a diuretic antihypertensive agent.

Glycovir, also known as SC-49483, is an anti-HIV prodrug. Glycovir is an alpha-glucosidase-1 inhibitor, and a candidate anti-HIV agent targeted against viral glycoprotein processing in host cell endoplasmic reticulum.

ZEN-2759 is BRD4(BD1) inhibitor.

Tacrolimus, also known as FK-506, is an immunosuppressive drug used mainly after allogeneic organ transplant to reduce the activity of the patient's immune system and to lower the risk of organ rejection. It is also used in a topical preparation in the treatment of atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, TH2-mediated diseases such as Kimura's disease, and the skin condition vitiligo. FK-506 is a macrolide isolated from the fungus Streptomyces tsukubaensis.

Axitirome, also known as CGS26214, is a highly selective thyromimetic and a synthetic cholesterol-lowering agent (HMG CoA reductase inhibitor) shown to be active in the rat, dog and monkey. CGS 26214 is a racemic compound, which is consisted of two equipotent chiral components CGS 28934(-) and CGS 28935(+). CGS 26214, virtually devoid of cardiovascular effects, has potent cholesterol-lowering activity in several models, reduces post-prandial response to a fat load in rats and markedly lowers Lp(a) concentrations in monkeys.

ATC0175 is a novel nonpeptidic and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.

Irgacure 651 is a photoinitiator to enhance the polymer degradation. It was found that the addition of the Irgacure 651 to PMMA accelerated|the photooxidative degradation, particularly at the early stages of exposure. The efficiency of formation of chromophoric groups in PMMA in the presence of the Irgacure initiator was significantly greater than in pure polymer. This suggests that the free-radical products of the initiator photolysis (mainly benzoyl radicals) are able to abstract hydrogen atoms from PMMA molecules.

Alentemol, also known as U-66444B and alentamol, is a selective dopamine autoreceptor agonist described as an antipsychotic. Chromosomal breakage following treatment of CHO-K1 cells in vitro with U-68,553B is due to induction of undercondensation of heterochromatin.

Alifedrine, also known as D13625, is a positive inotropic agent. Alifedrine moderately reduces the severity of ischaemia and reperfusion-induced ventricular arrhythmias. Alifedrine has an unusual and useful spectrum of pharmacological activity in that it combines antiarrhythmic activity with an ability to improve cardiac function. Alifedrine in the tested model markedly improved left ventricular function by balanced stimulation of the myocardium and reduction of pre- and afterload.

BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription.

BGP-15 is a novel poly(ADP-ribose) polymerase inhibitor - protects against nephrotoxicity of cisplatin without compromising its antitumor activity. BGP-15 also inhibits caspase-independent programmed cell death in acetaminophen-induced liver injury. Moreover, BGP-15 was found to prevent imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases.

Obatoclax, also known as GX 015-070, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon.

BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inhibited CDK2 at concentrations lower than 1 micromol/L, with CDK2 being inhibited 35-fold less potently (IC(50) 880 nmol/L) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo.

Antalarmin is a CRF-1 antagonist. By blocking CRF-1 activity the release of ACTH is reduced, and chronic stress is decreased in response to chronic stress. Antalarmin could be useful in reducing the adverse health consequences of chronic stress in humans, as well as treating anxiety, depression, and drug addiction.

Atevirdine, also known as U-87201, is a non-nucleoside reverse transcriptase inhibitor that has been studied for the treatment of HIV. Atevirdine has been shown to have significant anti-HIV RT activity in vitro, it inhibits HIV-1 replication in infected peripheral blood leukocyte cultures at a 50% inhibitory concentration of 1 nM and a concentration which is cytotoxic to 50% of cells of 100 μM and also inhibits completely the formation of syncytia in human T-cell leukemia virus type III-infected MT-2 cells at 2 μM.

Avitriptan, also known as BMS-180048, is a selective 5-HT1-like receptor agonist. Avitriptan is an effective compound for the treatment of migraine headaches with a prolonged duration of response. Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells.

K-604 is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor. K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. 102.85 μ M against human ACAT1 and ACAT2, respectively) and acyl-CoA-competitive (Ki = 378 nM against oleoyl-coA) manner.

Chlorthenoxazine is a non-steroidal anti-inflammatory drug (NSAID).

SHR1653 is a highly potent and selective oxytocin receptor (OTR) antagonist with improved blood-brain barrier penetration, which might be beneficial for the treatment of CNS-related PE.