5-Methyl-2'-O,4'-C-methylenecytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells[1].
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
Levosimendan(OR1259) is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.Target: OthersLevosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure. Levosimendan is an inodilator indicated for the short-term treatment of acutely decompensated severe chronic heart failure, and in situations where conventional therapy is not considered adequate. Levosimendan has shown preliminary positive effects in a range of conditions requiring inotropic support, including right ventricular failure, cardiogenic shock, septic shock, and Takotsubo cardiomyopathy [1]. The cardiovascular effects of levosimendan are exerted via more than an isolated drug-receptor interaction, and involve favorable energetic and neurohormonal changes that are unique in comparison to other types of inodilators [2]. Levosimendan might reduce mortality in cardiac surgery and cardiology settings of adult patients [3].
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1][2].
Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
Oleanolic acid-3-O-glucosyl(1-2)xylyl(1-3)glucosiduronic acid is a nature occurring triterpene saponin[1].
DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin, is an albumin binding prodrug.
Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Sodium lauryl sulfoacetate is a solid anionic surfactant of vegetable origin[1]. Sodium lauryl sulfoacetate is an immunoadjuvant. Anti-immunosuppressive effect[2].
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility[1].
2-Methoxy-4-vinylphenol (2M4VP), a naturally Germination inhibitor, exerts potent anti-inflammatory effects[1][2].
Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo[1]. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis[1][2].
FWM-5 is a potent NSP13 helicase inhibitor. SARS-COV-2 NSP13 helicase enzyme plays crucial role in the virus life cycle. FWM-5 has the potential for the research of infection diseases[1].
Tetradehydropodophyllotoxin possesses antifungal activity[1].
2’,3’,5’-Tri-O-acetyl-6-S-methyl-6-thio-guanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
Posaconazole-D4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].
3-Azidopropionic Acid Sulfo-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Mycothiol is a major low molecular-mass thiol that exists in mycobacteria. Mycothiol is an intracellular reducing agent[1].
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is a disaccharide of xylose monomers with a β-1, 4 bond between monomers[1].
H-D-MeAla-EtVaI-VaI-MeLeu-AIa-D-AIa-MeLeu-MeLeu-MeVaI-MeBmt(OAc)-Abu-O-CH2-CH2-NHMe is a nonimmunosuppressive cyclosporin A derivative. H-D-MeAla-EtVaI-VaI-MeLeu-AIa-D-AIa-MeLeu-MeLeu-MeVaI-MeBmt(OAc)-Abu-O-CH2-CH2-NHMe has the potential for the research of congenital muscular dystrophy[1].
Propaquizafop is a phenoxyisopropionic acid herbicide and an acetyl-coA carboxylase inhibitor[1][2].
Guajadial, a caryophyllene-based meroterpenoid, has anti-estrogenic and anticancer effect. Guajadial reverses multidrug resistance in cancer. Guajadial can be isolated from Psidium guajava leaves[1][2].
Charantin is a steroidal saponin isolated from Momordica charantia, and has insulin-like activity, by increasing the release of insulin and slowing down gluconeogenesis. Charantin can against GSK-3[1].
Eliglustat hemitartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].
Afzelin (Kaempferol-3-O-rhamnoside) is is a flavonol glycoside found in Houttuynia cordata Thunberg and is widely used in the preparation of antibacterial and antipyretic agents, detoxicants and for the treatment of inflammation. Afzelin attenuates the mitochondrial damage, enhances mitochondrial biogenesis and decreases the level of mitophagy-related proteins, parkin and PTEN-induced putative kinase 1. Afzelin improves the survival rate and reduces the serum levels of alanine aminotransferase and pro-inflammatory cytokines in D-galactosamine (GalN)/LPS -treated mice[1].
Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.