ml 364

ML364 是一种泛素蛋白特异性肽酶 (USP2) 抑制剂，具有抗增殖活性，IC50为1.1 μM，Kd=5.2 μM。它可直接结合 USP2，诱导细胞周期蛋白 D1 降解增加并导致细胞周期停滞。它增加线粒体活性氧水平，降低胞内 ATP 含量，可用于乳腺癌的研究。

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)

Monocerin is a fungal metabolite that has been found inF. larvarumand has diverse biological activities.1,2,3It is active against the bacteriaE. coliandB. megaterium, the phytopathogenic fungusM. violaceum, and the algaC. fuscain an agar diffusion assay when used at a concentration of 50 μg/disc.1Monocerin (17.5 μg/ml) induces mortality in adultC. erythrocephala.2It reduces root elongation in pre-germinatedS. halepenseseeds when used at a concentration of 33 ppm.3 1.Zhang, W., Krohn, K., Draeger, S., et al.Bioactive isocoumarins isolated from the endophytic fungus Microdochium bolleyiJ. Nat. Prod.71(6)1078-1081(2008) 2.Claydon, N., Grove, J.F., and Pople, M.Insecticidal secondary metabolic products from the entomogenous fungus Fusarium larvarumJ. Invertebr. Pathol.33(3)364-367(1979) 3.Robeson, D.J., and Strobel, G.A.Monocerin, a phytotoxin from Exserohilum turcicum (Drechslera turcica)Agr. BioI. Chem.46(11)2681-2683(1982)