|S1186||BIBR 1532||<1 mg/mL||66 mg/mL||3 mg/mL|
|S1319||Costunolide||<1 mg/mL||47 mg/mL||1 mg/mL|
|S2250||(-)-Epigallocatechin Gallate||23 mg/mL||72 mg/mL||83 mg/mL|
|S4981||Cyclogalegenol||<1 mg/mL||98 mg/mL||19 mg/mL|
|S3894||Cycloastragenol||-1 mg/mL||98 mg/mL||-1 mg/mL|
|S8118||RHPS 4 methosulfate||<1 mg/mL||91 mg/mL||<1 mg/mL|
BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase were observed at concentrations vastly exceeding the IC50 for telomerase.
(E, F)The cells were not treated or treated with BIBR1532 before wounds were made. Relative ratio of wound closure per field was shown. (G, H) KrasG12D and KrasG12V-induced migration ability of lung cancer cells was inhibited by BIBR1532 in Transwell invasion assay. Numbers of invasive cells in 10 fields were counted. Magnification: ×200. Representative pictures were shown. Values were the mean of 3 determinations ± SEM (one-way ANOVA, *p < 0.05, **p < 0.01).
Costunolide, a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM.
(-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
(a) Huh7 cells were incubated with HCVcc of JFH-1 for 2 h before overlaying with 1% agarose dissolved in culture medium or with AR3A anti-E2 neutralizing antibodies, in the presence of 20 μg/ml SZA. EGCG (50 μM) was introduced as a positive control. At 48 h post-infection, infected cells were quantified by IF. Nuclei were stained with DAPI. (b) Numbers of cells per positive colony were determined in 15 foci.
Cyclogalegenol, the aglycone derivative of astragaloside A, is found in various species of Astragalus and may activate telomerase.
Cycloastragenol is a saponin comprising a group of oil glucosides naturally present in a number of plants. It is a potent telomerase activator in neuronal cells.
RHPS4 is a potent inhibitor of Telomerase at submicromolar.