DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs)[1].
Guattegaumerine is a bisbenzylisoquinoline alkaloid with antimitotic, cytotoxic and neuroprotective activities[1].
Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties[1].
2-mercaptoethane sulfonate (Mesna), is a synthetic small molecule, widely used as a systemic protective agent against chemotherapy toxicity, but is primarily used to reduce hemorrhagic cystitis induced by cyclophosphamide.IC50 Value: 182 mM (decreased superoxide anion production stimulated with PMA (tetradecanoylphorbol acetate) in PMN in-vitro); 70mM (inhibited H2O2 production) [3]Target: in vitro: MESNA had no effect on the qualitative and quantitative characteristics of the indicated processes in both the types of the doxorubicin sensitive cells. The combined use of doxorubicin and phosphamide or cyclophosphane the use of MESNA for lowering the urotoxic action of oxazophosphorines had no effect on the biological efficacy of doxorubicin [4].in vivo: AMH-positive follicles were significantly decreased after cisplatin administration, which was significantly reversed when mesna was co-administered with cisplatin. The end product of lipid peroxidation, malondialdehyde (MDA), was significantly increased, but the anti-oxidative enzymatic activity of superoxide dismutase (SOD) and glutathione (GSH) were significantly decreased in cisplatin groups when compared with NS group. In contrast, after co-administration of cisplatin with mesna, MDA was significantly decreased whereas the activity of SOD and the concentration of GSH were increased. Moreover, mesna did not decrease the anti-tumor property of cisplatin in HePG2 cell lines [2]. After head trauma, tissue malondialdehyde levels increased; these levels were significantly decreased by MESNA administration. Caspase-3 levels were increased after trauma, but no effect of MESNA was determined in caspase-3 activity [1].Clinical trial: Effects of Mesna on Homocysteine in Kidney Failure . Phase2
Ezetimibe phenoxy glucuronide-D4 (Ezetimibe glucuronide-D4) is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity[1]. Ezetimibe is a potent cholesterol absorption inhibitor[2].
Fexofenadine Impurity F is the impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial[1].
Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC50 of 6.3 μM[1].
5'-O-DMT-5-Ethynyl-2'-deoxyuridine 3'-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
(Z)-ONO 1301 is the inactive isomer of ONO 1301 (HY-106961), and can be used as an experimental control. ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig[1][2][3].
Amuvatinib hydrochloride (MP470 hydrochloride) is a multi-targeted receptor tyrosine kinases inhibitor, which inhibits c-Kit (D816V), c-Kit (D816H), c-Kit (V560G), c-Kit (V654A), PDGFRα (D842V), and PDGFRα (V561D) with IC50s of 950 nM, 10 nM, 34 nM, 127 nM, 81 nM, and 40 nM, respectively[1]. Antineoplastic activity[2].
MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
7'-Hydroxy ABA (7'-OH ABA) is a metabolite of Abscisic acid (Abscisic acid) through hydroxylation of the 7′-carbon atom of Abscisic acid. 7'-Hydroxy ABA exhibits significant hormonal activity[1].
Purpurin 18 methyl ester, a chlorophyll-a derivative, and is a photosensitizer that can be used in photodynamic therapy (PDT). Purpurin 18 methyl ester has photodynamic activity to induce cancer cell death[1].
Suomilide inhibits human trypsin-2 and -3, with IC50 values of 4.7 and 11.5 nM, respectively, while trypsin-1 is inhibited with an IC50 of 104 nM.
Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility[1][2][3].
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
m-PEG6-(CH2)6-Phosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1-Heptadecanoyl-2-myristoleoyl-sn-glycero-3-phospho- L-serine-d5 (sodium) is deuterium labeled 1-Heptadecanoyl-2-myristoleoyl-sn-glycero-3-phospho- L-serine (sodium).
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
Aeide-C1-NHS ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[1][2][3]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[4].
Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole has anti-infection and anti-cancer effects[1][2][3].
MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is an ADC linker that can be combined with the cytotoxic Camptothecin (HY-16560) to form ADC-related drug-linker conjugates (Drug-Linker Conjugates for ADC ).MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is conjugated to Camptothecin, which can further bind to the antibody Trastuzumab (HY-P9907) to form Antibody-Drug Conjugates (ADCs)[1].
N-Fmoc-4-(tert-butoxycarbonylmethoxy)-L-phenylalanine is a phenylalanine derivative[1].
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4[1].
CC-885-CH2-PEG1-NH-CH3 is a neoDegrader that can be used in the synthesis of Antibody neoDegrader Conjugate (AnDC)[1][2].
6-Methylcoumarin is a synthetic fragrance widely used in cosmetics.
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption. Sequence: Cys-Ser-Asn-Leu-Ser-Thr-Cys-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-NH2(Disulfide bridge: Cys1-Cys7).
Aspergillopepsin I (Aspergillus acid protease) is an aspartic endopeptidase that catalyses the hydrolysis of peptide bonds in proteins, with broad specificity[1].