e 260

E260 (Fer and FerT inhibitor) 是Fer FerT 激酶抑制剂。

Benastatin B is a polyketide synthase-derived benastatin that has been found in Streptomyces and has diverse biological activities. It inhibits glutathione S-transferase (GST; Ki = 3.7 µM for the rat liver enzyme).2 Benastatin B also inhibits the transglycosylase activity of A. baumannii, C. difficile, E. coli, and S. aureus recombinant penicillin-binding proteins (PBPs; IC50s = 16, 53.3, 30.7, and 31.6 µM, respectively).3 It is active against several bacteria, including methicillin-resistant S. aureus (MRSA; MIC = 3.12 µg ml).

Kobe2602 是 Ras-Raf 相互作用抑制剂，具有抗癌化疗活性。它抑制 H-Ras·GTP 与 c-Raf-1 RBD 结合的Ki 值为 149 μM。

Kobe2601 is a Kobe0065 and Kobe02602 water-soluble analog. It displays inhibitory activity towards Ras-Raf binding.

(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)