Valylvaline is a bioactive chemical.

Caleprunin B, also known as Eupatarone, is a benzofuran from Ruscus aculeatus L.

Seladelpar, also known as MBX-8025 and RWJ-800025, is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist. MBX-8025 may have potential use for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis.

Daniquidone, also known as Batracylin, is a water-insoluble heterocyclic amide with potential antineoplastic activity. Daniquidone inhibits topoisomerases I and II, thereby inhibiting DNA replication and repair, and RNA and protein synthesis. The acetylated form of daniquidone is highly toxic and is capable of inducing unscheduled DNA synthesis; rapid acetylators are more likely to experience toxicity with this agent.

Rosmanol is a natural polyphenol from the herb rosemary (Rosmarinus officinalis L.) with high antioxidant activity.

Difetarsone is an antiprotozoal agent. Various studies have shown it to be particularly effective against Trichuris trichiura, commonly known as the whipworm. It has also been used to treat Entamoeba histolytica infections. Prior to the drugs use in the early 1970s, there were few effective treatments for this infection. Difetarsone often has minor side effects, which include rashes, nausea and vomiting. It has also resulted in angioedema in at least one known case.

GSK-J4 is a cell permeable, potent and selective histone demethylase. GSK-J4 is a prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF).

AC430 is a potent and specific small molecule inhibitor of janus kinase 2 (JAK2), which has been implicated as a target for therapy in both oncology and autoimmune disease. AC430 is currently being developed by Ambit. In preclinical studies, AC430 has exhibited potency against JAK2 and V617F mutated JAK2 in cell-based models that is at least equivalent to, and in most cases superior to, competing JAK2 inhibitors. In preclinical oncology and autoimmune models, AC430 is well tolerated and has significant efficacy at oral doses as low as 10 mg/kg/day.

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.