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.

Gemcitabine monophosphate disodium salt, also called GemMP, is a monophosphate derivative of Gemcitabine. Gemcitabine (Gem) is a deoxycytidine analog that is effective against pancreatic cancer and other malignancies following conversion to the 5'-O-mono-, di- and tri-phosphate forms. GemMP decreased tumor cell growth at concentrations ranging from 1 to 50 nM. GemMP is a potent cytotoxic agent that serves to induce apoptosis in association with increased Fas expression in cultured thyroid cancer cell lines. (Anticancer Res. 2000 Sep-Oct;20(5A):2915-22). Note: Current batch has purity ~ 90%.

Azalanstat is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Pravibismane, also known as BisEDT, MBN 101, is a novel broad-spectrum topical anti-infective and an antibacterial agent against a broad range of gram-positive and gram-negative pathogens. Pravibismane inhibited adherence of P. aeruginosa to 16HBE14o- cells by 28% and to a collagen matrix by 53%. Pravibismane-treated bacteria were also 100-fold more sensitive to serum bactericidal activity.

Bobcat339 is a novel cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2). Bobcat339 has mid-μM inhibitor activity against TET1 and TET2, but does not inhibit the DNA methyltransferase, DNMT3a. These new molecular tools will be useful to the field of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription.

Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50/IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 +/- 0.08 micromol/l after 24 h) than As(2)O(3) (IC50 = 1.60 +/- 0.23 micromol/l after 24 h) or melarsoprol (IC50 = 1.44 +/- 0.08 micromol/l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.

Eravacycline, also known as TP-434, a novel antibiotics. Eravacycline showed potent broad-spectrum activity against 90% of the isolates (MIC90) in each panel at concentrations ranging from ≤0.008 to 2 μg/ml for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia (MIC90 values of 32 μg/ml for both organisms). The antibacterial activity of eravacycline was minimally affected by expression of tetracycline-specific efflux and ribosomal protection mechanisms in clinical isolates. Furthermore, eravacycline was active against multidrug-resistant bacteria. Eravacycline has the potential to be a promising new intravenous (i.v.)/oral antibiotic for the empirical treatment of complicated hospital/health care infections and moderate-to-severe community-acquired infections.

Atigliflozin, also known as AVE 2268, is an antihyperglycaemic drug candidate.

Nirogacestat, also known as PF-03084014, is a potent and selective gamma secretase (GS) inhibitor with potential antitumor activity. PF-03084014 binds to GS, blocking proteolytic activation of Notch receptors. Nirogacestat enhances the Antitumor Effect of Docetaxel in Prostate Cancer. Nirogacestat enhances docetaxel-mediated tumor response and provides a rationale to explore GSIs as adjunct therapy in conjunction with docetaxel for men with CRPC (castration-resistant prostate cancer).

Sofinicline, also known as ABT-894 and A-422894, is a novel nicotinic acetylcholine receptor agonist under development for the treatment of attention-deficit/hyperactivity disorder. Sofinicline appears to be well tolerated and showing efficacy similar to that of atomoxetine.

JQKD82, also known as PCK82, is a cell-permeable and selective KDM5 inhibitor (MM.1S cells, IC50 = 0.42 uM). JQKD82 increases histone H3K4me3 but paradoxically inhibits downstream MYC-driven transcriptional output in vitro and in vivo. JQKD82 is a useful tool compound to block KDM5A function as a potential therapeutic strategy for MM. QKD82 is a more stable ester of KDM5-C49 that is able to deliver the active molecule KDM5-C49 to cells more efficiently

WUN40378 is compound first reported in PCT Int. Appl. (2019), WO 201909959, in which it was described as CBFβ-​RUNX1 inhibitor. WUN40378 is very similar to Ro 5-3335 but with an F instead of Cl. WUN40378 is also analog of Ro 24-7429. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

Dobutamine is a sympathomimetic drug used in the treatment of heart failure and cardiogenic shock. Its primary mechanism is direct stimulation of β1 receptors of the sympathetic nervous system.

Lomibuvir, also known as VX-222, VCH-222 and VX22, is an nonnucleoside NS5B polymerase inhibitor. VX-222 inhibits the 1b/Con1 HCV subgenomic replicon, with 50% effective concentrations (EC(50)s) 5 nM. VX-222 binds to the HCV polymerase with dissociation constants of 17 nM. In phase 1 and 2 clinical studies, VX-222 demonstrated effective antiviral efficacy, with substantial reductions in plasma HCV RNA in patients chronically infected with genotype 1 HCV.

Treprostinil is a vasodilator that is used for the treatment of pulmonary arterial hypertension. Treprostinil is a chemically stable prostacyclin analog. Its principal pharmacologic action is direct vasodilation, which causes reduction of pulmonary and systemic arterial pressure, reducing right and left ventricular afterload; therefore improves the cardiac output. It also has an antiplatelet effect.

Isavuconazole (BAL4815; trade name Cresemba) is a triazole antifungal drug. Its prodrug, isavuconazonium sulfate (BAL8557), was granted approval by the U.S. Food and Drug Administration (FDA) on March 6, 2015. Isavuconazole has been approved for treatment of invasive aspergillosis and invasive mucormycosis in adults ages 18 years and older. Both infections are caused by mold and fungi common to the environment, and occur in individuals who are immunosuppressed or have other complicating conditions, such as diabetes or lung disease.

NADPH, the reduced form of NADP+, is used in anabolic reactions (such as lipid and nucleic acid synthesis) as a reducing agent and cofactor.

NADPH, tetrasodium salt is the sodium salt form of NADPH, which the reduced form of NADP+. NADPH is used in anabolic reactions (such as lipid and nucleic acid synthesis) as a reducing agent and cofactor.

Abediterol, also known as LAS100977, is a novel potent, long-acting inhaled β(2)-adrenoceptor agonist in development for the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows subnanomolar affinity for the human β(2)-adrenoceptor and a functional selectivity over β(1)-adrenoceptors higher than that of formoterol and indacaterol in both a cellular model with overexpressed human receptors and isolated guinea pig tissue. Abediterol is a full agonist at the human β(2)-adrenoceptor (E(max) = 91 ± 5% of the maximal effect of isoprenaline). The potency and onset of action that abediterol shows in isolated human bronchi (EC(50) = 1.9 ± 0.4 nM; t½ onset = 7-10 min) is not significantly different from that of formoterol, but its duration of action (t½ ∼ 690 min) is similar to that of indacaterol.

NADPH Cy4N also known as NADPH, cyclohexyl ammonium salt is the ammonium salt form of NADPH, which the reduced form of NADP+. NADPH is used in anabolic reactions (such as lipid and nucleic acid synthesis) as a reducing agent and cofactor.

NADH is the reduced form of NAD, or nicotinamide adenine dinucleotide. NADH is used as a reducing agent to donate electrons in metabolic reactions.

Exeporfinium, also known as XF-73, is an anti-microbial which works via weakening bacteria cell walls. Exeporfinium chloride is a potential treatment for methicillin-resistant Staphylococcus aureus (MRSA) and possibly Clostridium difficile. Exeporfinium chloride has completed a phase I clinical trial for nasal decolonisation of MRSA—being tested against 5 bacterial strains. It seems unlikely to cause MRSA to develop resistance to it. Structurally it is a dicationic porphyrin.

KPI-10, also known as WQ3810, is a new compound currently being studied for its efficacy in the treatment of infections caused by multidrug-resistant bacteria. WQ-3810 demonstrated high potent activity against the antimicrobial-resistant pathogens tested. WQ-3810 (MIC(90)=4 mg/L and 0.06 mg/L, respectively) was also more active than ciprofloxacin (64 mg/L and 2 mg/L) and levofloxacin (32 mg/L and 2 mg/L). Furthermore, WQ-3810 was the most potent among the fluoroquinolones tested against meticillin-resistant Staphylococcus aureus (MRSA) and Neisseria gonorrhoeae, including FQR isolates.