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Meisoindigo(Natura-¦Á; N-Methylisoindigotin; Dian III), a derivative of Indigo naturalis, might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML).

June 21, 2017

prudect name : Meisoindigo(Natura-¦Á; N-Methylisoindigotin; Dian III), a derivative of Indigo naturalis, might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML).Meisoindigo Synonyms: CAS NO: 97207-47-1Molecular Formula: C17H12N2O2Molecular Weight:…

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Moxifloxacin is a fourth-generation quinolone broad-spectrum antibiotics, the treatment of severe respiratory tract infections¡£

prudect name : Moxifloxacin is a fourth-generation quinolone broad-spectrum antibiotics, the treatment of severe respiratory tract infections¡£Moxifloxacin Synonyms: CAS NO: 151096-09-2Molecular Formula: C21H24FN3O4Molecular Weight: 401.44Purity: 99%Solubility: Storage: −20°C 2 years…

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MK-2206, a highly selective non-ATP competitive allosteric Akti, has nM IC50 and broad preclinical antitumor activity. MK-2206 is a potent allosteric Akt inhibitor with IC50 at 8 nm, 2 mM, 65 mM for Akt1, Akt2 and Akt3 respectively. 1 hr treatment of 1 ¦ÌM MK-2206 abolished Akt phosphorylation in U87MG cells. MK-2206 treatment abolished IR-induced Akt phosphorylation. Moreover, treatment with MK-2206 also increased the radiosensitivity of U87MG cells.

prudect name : MK-2206, a highly selective non-ATP competitive allosteric Akti, has nM IC50 and broad preclinical antitumor activity. MK-2206 is a potent allosteric Akt inhibitor with IC50 at 8…

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MDV3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also induces tumour cell apoptosis, and has no agonist activity.

prudect name : MDV3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also…

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Midostaurin(pkc412) may suppress tumor growth by inhibiting tumor angiogenesis (via its effects on the VEGF receptor tyrosine kinases) in addition to directly inhibiting tumor cell proliferation (via its effects on PKCs). This anti-angiogenic action may contribute to the antimetastatic and broad antitumor activity displayed by midostaurin(pkc412), as well as the synergy with cytotoxic agents, including doxorubicin, cyclophosphamide, cisplatin and gemcitabine. When given orally, the maximally tolerated dose for midostaurin(pkc412) is >300 mg/kg.

prudect name : Midostaurin(pkc412) may suppress tumor growth by inhibiting tumor angiogenesis (via its effects on the VEGF receptor tyrosine kinases) in addition to directly inhibiting tumor cell proliferation (via…

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MK-0812 is chemokine receptor CCR-2 antagonist

prudect name : MK-0812 is chemokine receptor CCR-2 antagonistMK 0812 Synonyms: CAS NO: 624733-88-6Molecular Formula: C24H34F3N3O3Molecular Weight: 469.54Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528958

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Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1).

prudect name : Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1).Mdivi-1 Synonyms: CAS NO: 338967-87-6Molecular Formula: C15H10Cl2N2O2SMolecular Weight: 353.22Purity: 98%…

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Motesanib (AMG-706) is an orally bioavailable diphosphate salt of a multiple receptor tyrosine kinase inhibitor with potential antineoplastic activity[1]. This reagent selectively targets and inhibits VEGFR1/2/3(IC50: 2 nM /3 nM /6 nM), PDGFR (84nM), kit (8nM), and Ret (59nM)receptors, thereby inhibiting angiogenesis and cellular proliferation. Oral administration of AMG 706 potently inhibited VEGF-induced angiogenesis in the rat corneal model and induced regression of established A431 xenografts

prudect name : Motesanib (AMG-706) is an orally bioavailable diphosphate salt of a multiple receptor tyrosine kinase inhibitor with potential antineoplastic activity[1]. This reagent selectively targets and inhibits VEGFR1/2/3(IC50: 2…

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Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM. In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.Aristoff, P.A., Johnson, P.D., and Harrison, A.W. Synthesis of 9-substituted carbacyclin analogues. J Org Chem 48 5341-5348 (1983). Murata, T., Ushikubi, F., Matsuoka, T., et al. Altered pain perception and inflammatory response in mice lacking prostacyclin receptor. Nature 388 678-682 (1997). Cheng, Y., Austin, S.C., Rocca, B., et al. Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 296 539-541 (2002). Cui, Y., Kataoka, Y., Satoh, T., et al. Protective effect of prostaglandin I2 analogs on ischemic delayed neuronal damage in gerbils. Biochem Biophys Res Commun 265 301-304 (1999). McLaughlin, V.V., Genthner, D.E., Panella, M.M., et al. Reduction in pulmonary vascular resistance with long-term epoprostenol (prostacyclin) therapy in primary pulmonary hypertension. N Engl J Med 338 273-277 (1998). Kuwano, K., Hashino, A., Asaki, T., et al. 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J Pharmacol Exp Ther 322(3) 1181-1188 (2007).Kuwano, K., Hashino, A., Noda, K., et al. A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active form, {4-[5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid (MRE-269), on rat pulmonary artery. J Pharmacol Exp Ther 326(3) 691-699 (2008).

prudect name : Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on…

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Monomethyl auristatin E (MMAE; Vedotin) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin.

prudect name : Monomethyl auristatin E (MMAE; Vedotin) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation…

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