Ansamitocin P3' is an isomer of Ansamitocin P-3 or iso-Ansamitocin P-3 , is a natural product. Ansamitocin P-3' showed potential antineoplastic and antimitotic activity. Ansamitocin -' binds to tubulin and inhibits vinblastine-induced spiral formation.

Cefteram is a cephalosporin antibiotic. Its prodrug is Cefteram Pivoxil, which is used in the treatment of infections caused by bacteria. It works by killing bacteria or preventing their growth. Cefditoren pivoxil is also used to treat some throat and lung infections, including bronchitis and tonsillitis. It is also used to treat some skin infections.

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).

RA371, a derivative of PTP1B-IN-8 (CAS#919091-61-5), is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor

NG-25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer.

P7C3A20-analog, as known as defluoro-P7C3-A20, is a structural analogue of P7C3-A20. Compared to P7C3-A20 structure, P7C3-A20 analog has no fluorine atom in the 1,3-diaminopropane-bridge. P7C3-A20 analog was synthesized by mistake during a process to make P7C3-A20. The bioactivity of P7C3-A20 analog is unknown. P7C3-A20 analog may be used for research to compare with P7C3-A20. P7C3-A20 is a proneurogenic, neuroprotective agent. P7C3-A20 displayed increased activity and an improved toxicity profile compared to P7C3. P7C3-A20 demonstrated greater proneurogenic efficacy than a wide spectrum of currently marketed antidepressant drugs. P7C3-A20 showed neuroprotective properties in rodent models of Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury and age-related cognitive decline.

AG-045572 is a selective gonadotropin-releasing hormone (GnRH) receptor antagonist that suppresses testosterone and luteinising hormone (LH) levels in vivo.

GNF2133 is a potent and selective DYRK1A inhibitor (IC50 = 6 nM). In vitro, GNF2133 is able to proliferate both rodent and human β-cells. In vivo, GNF2133 demonstrated significant dose-dependent glucose disposal capacity and insulin secretion in response to glucose-potentiated arginine-induced insulin secretion (GPAIS) challenge in rat insulin promoter and diphtheria toxin A (RIP-DTA) mice.

Mupirocin is an antibiotic and bacterial metabolite that has been found in P. fluorescens. It is bacteriostatic against S. aureus (MIC = 0.05 µg/ml) and active against skin wound clinical isolates of methicillin-resistant S. aureus (MRSA; MICs = 1-4 µg/ml). Mupirocin inhibits MRSA and P. aeruginosa biofilm formation in vitro.4 It inhibits bacterial cell wall isoleucyl-tRNA synthetase, slowing bacterial growth. Topical administration of Mupirocin (2% v/v) reduces the number of wound colony forming units (CFUs) in a mouse model of MRSA skin infection. Lithium mupirocin as been used to study mupirocin resistance in staphylococcus aureus and in mycoplasma susceptibility studies.

PYR-5084, CAS#59435-08-4, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs.

Quipazine dimaleate is a selective 5-HT3 receptor agonist that also displays antagonist activity at peripheral 5-HT3 receptors. [3H]-Quipazine labels 5-HT3 sites in the cortical membranes.

ICI-204448 is a potent and peripherally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching effects. It is used in research to distinguish centrally from peripherally mediated kappa opioid receptor effects.

TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells

Dalbavancin is a novel second-generation lipoglycopeptide antibiotic. It belongs to the same class as vancomycin, the most widely used and one of the few treatments available to patients infected with methicillin-resistant Staphylococcus aureus (MRSA). Dalbavancin is a semisynthetic lipoglycopeptide that was designed to improve upon the natural glycopeptides currently available, vancomycin and teicoplanin. It possesses in vitro activity against a variety of Gram-positive pathogens including MRSA and methicillin-resistant Staphylococcus epidermidis (MRSE).

Bupropion, also known as amfebutamone and BW 323, is a norepinephrine–dopamine reuptake inhibitor (NDRI) and a nicotinic receptor antagonist. However, its effects on dopamine are weak and clinical significance is contentious. Chemically, bupropion is an aminoketone that belongs to the class of substituted cathinones and more generally that of substituted amphetamines and substituted phenethylamines.

JBJ-04-125-02 is a mutant-selective EGFR allosteric inhibitor with potential anticancer activity. As a single agent, it can inhibit cell proliferation and EGFRL858R/T790M/C797S signaling in vitro and in vivo. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, a more effective inhibition of cellular growth, and an increased efficacy in vitro and in vivo compared with either single agent alone.

JHN07588, also known as MMP-2/MMP-9 inhibitor I, is a potent inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9. It acts by binding zinc at the active site of these MMPs. This compound has been used to elucidate the roles of MMP-2 and MMP-9 in diverse systems, including mammary epithelial cell transformation, neuronal dysfunction, lymphocyte recruitment, and progressive hereditary kidney disease. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

Tarloxotinib bromide, also known TH-4000 or PR-610, is a prodrug designed to selectively release a covalent (irreversible) EGFR tyrosine kinase inhibitor under severe hypoxia, a feature of many solid tumors. Tarloxotinib has the potential to effectively shut down aberrant EGFR signaling in a tumor-selective manner, thus potentially avoiding or reducing the systemic side effects associated with currently available EGFR tyrosine kinase inhibitors.

YCN47284 is an aromatic guanylhydrazone compounds with antimalarial activity. YCN47284 was first reported in WO 9621450. YCN47284 inhibited P. falciparum growth with IC50 = 0.075 μM to >10 μM as reported in US 20030186993. 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).

Artilide, also known as U88943 or U88943E, is a drug used for the treatment of cardiac arrhythmias. Artilide is a class III antiarrhythmic which is structurally-related to ibutilide and d,l-sotalol. Artilide had demonstrated inducibe ventricular arrhythmias prior to treatment. This antiarrhythmic action was associated with significant increases in ventricular refractoriness and monophasic action potential duration. Lower doses of artilide tended to reduce the incidence of spontaneous ventricular arrhythmias but these effects were not significant. These results are consistent with the concept that spontaneous and pacing induced ventricular arrhythmias result from different mechanisms, and that class III anti-arrhythmic agents are more effective in suppressing induced ventricular tachycardia due to reentry than spontaneous arrhythmias which result from nonreentrant mechanisms.

Befiperide, also known as DU-29325, is a substituted piperazine that has agonist activity at serotonin1 receptors.

BXT 51072, also known as ALT-2074, belongs to a class of drugs called "glutathione peroxidase mimics." BXT-51072 works by imitating a substance produced in various tissues in the body, which prevents damage of the heart and blood vessels. The intraocular injection of BXT-51072 protected axotomized neurons at doses in a narrow (tenfold) range. It also reduced the deleterious effects of intraocular tert-butyl hydroperoxide, an inducer of lipid peroxidation, and diminished the excitotoxic degeneration induced by N-methyl-D-aspartate. However, BXT-51072 did not noticeably reduce naturally occurring cell death.

MA-VAL-ALA-PAB-OH is a usefully ACD-linker, which was reported in JACS 2020, 142, pp12890-12895.

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, is a GABA receptor modulator. It binds to GABAA and GABAB receptors and inhibits GABA uptake in rat brain synaptosomes. (R)-4-amino-3-hydroxybutyric acid is also a GABAC receptor agonist that induces currents in a patch-clamp assay using Xenopus oocytes expressing the human receptor. In vivo, (R)-4-amino-3-hydroxybutyric acid inhibits electrical discharges in the amygdala in a cat model of N-amidinobenzamide-induced seizures.

ACHP is an IκB kinase inhibitor that inhibits DNA binding activity of NF-κB, blocks NF-κB pathway in multiple myeloma cell lines, and induces cell growth arrest and apoptosis. It also inhibits STAT3 signaling in NSCLC in vitro.

BD-AcAc2 is a ketone ester with anti-obesity and anticonvulsant activities. Oral administration of BD-AcAc2 reduces body weight, food intake, and whole animal adiposity in mice fed an isocaloric diet. BD-AcAc2 increases the seizure threshold and blood levels of β-hydroxybutyrate in a rat model of seizures induced by pentylenetetrazole.

AZD-2207 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes mellitus and obesity.

Exametazime is a Diagnostic Aid (Regional Cerebral Perfusion Imaging). It is a radiopharmaceutical sold under the trade name Ceretec, and is used by nuclear medicine physicians for the detection of altered regional cerebral perfusion in stroke and other cerebrovascular diseases.

ORY1001, also known as RG-6016, is KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). ORY-1001 does not inhibit non-related histone modifiers. Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers (EC50 me2H3K4 and FACS CD11b <1nM). ORY-1001 induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells (EC50 <1nM).

AZD1446, also known as TC-6683, is a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. AZD1446 showed favorable pharmaceutical properties and in vivo efficacy in animal models has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions and had been evaluated in phase 2 clinical trials as a treatment for Alzheimer's disease.