Cytochalasin A is a cell-permeable fungal toxin and is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50 = 3 μM), inhibits actinpolymerization and interferes with microtubule assembly by reacting with sulfhy
Latrunculin A is a toxin isolated from the red sea sponge Latrunculia magnifica. Latrunculin A binds to actin monomers and it also inhibits polymerization of actin (Kds: 0.1, 0.4, 4.7 μM, and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin, and G-actin, re
19-O-Acetylchaetoglobosin A is a fungal metabolite originally isolated fromC. globosumthat has actinpolymerization inhibitory and cytotoxic activities.1,2It inhibits actinpolymerization in a cell-free assay when used at a concentration of 2 μM.219-O-Acetylchaetoglobosin A (3.2, 10, and 32 μg ml) is cytotoxic to HeLa cervical cancer cells.1 1.Umeda, M., Ohtsubo, K., Saito, M., et al.Cytotoxicity of new cytochalasans from Chaetomium globosumExperientia31(4)435-438(1975) 2.Sekita, S., Yoshihira, K., Natori, S., et al.Structure-activity relationship of thirty-nine cytochalasans observed in the effects on cellular structures and cellular events and on actinpolymerization in vitroJ. Pharmacobiodyn.8(11)906-916(1985)
Diminutol is a cell-permeable purine derivative that inhibits the NADP-dependent oxidoreductase, NQO1 (Ki = 1.72 μM), to destabilize microtubules and disrupt mitosis. At 50 μM, it directly affects tubulin polymerization in Xenopus egg extracts without interfering with the activity of Cdk1, DNA replication, or actinpolymerization.
Kibdelone C is a member of a family of natural heterocyclic polyketides first isolated from a soil actinomycete, Kibdelosporangium. Kibdelones have been described as having potent and selective cytotoxicity against a panel of human tumor cell lines, and kibdelone C has low nanomolar effectiveness in these assays. Kibdelone C disrupts the actin cytoskeleton without directly binding actin or affecting its polymerization in vitro.
Fluvoxketone is trifluoromethyl-substituted aryl ketone compound useful as an intermediate in the synthesis of Fluvoxamine, which is a selective serotonin reuptake inhibitor. In the synthesis of Fluvoxamine, the ketone carbonyl of Fluvoxketone is elaborated to an oxime.In vitro,the inhibitory effect of fluvoxamine on actinpolymerization was concentration dependent, and its IC50 was approximately 30 μM.In vivo,fluvoxamine treated EAE rats showed a decrease in IFN-γ serum levels and an increase in IL-4, pro- and anti-inflammatory cytokines respectively.
DMGF, also known as 7,7-dimethoxyagastisfavone, is a biflavonoid isolated from Taxus × media cv. Hicksii. DMGF induces apoptotic and autophagic cell death. DMGF could effectively attenuate the motility of B16F10 cells, and the results of real-time PCR revealed that DMGF also suppressed the expressions of matrix metalloproteinase-2 (MMP-2). MGF can inhibit the metastasis of highly invasive melanoma cancer cells through the down-regulation of F-actinpolymerization DMGF may be further developed to serve as a chemoprevention drug for patients with metastatic melanoma.
16-epiLatrunculin B, a stereoisomer of the actinpolymerization inhibitor latrunculin B, was initially isolated from the Red Sea sponge N. magnifica. At concentrations of 5-10 µg/ml, it disrupts microfilament activity in actin disruption assays and exhibits cytotoxic effects on mouse KA31T and NIH3T3 tumor cells, with GI50 values of 1 and 4 µg/ml, respectively. Furthermore, it shows antiviral activity against herpes simplex type 1 virus, with an ED50 of 1 µg/ml.
Inhibits neural Wiskott-Aldrich syndrome protein (N-WASP) by stabilizing the autoinhibited state of the protein. Blocks phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly (IC50 ~ 2 μM) but does not directly inhibit actinpolymerization