Verucopeptin

ATP6V1G, a subunit of the vacuolar H⁺-ATPase (v-ATPase)^[3].
Verucopeptin?(0-30 μM; 72 h) shows excellent antitumor activity against K562R cells, with an IC₅₀ of 388 nM, although these cells exhibit resistance to some other chemotherapeutic agents, such as Taxol and vincristine at concentrations of 10 μM^[3].
Verucopeptin?(0-1 μM) shows broad antiproliferative activity, with IC₅₀ values of less than 100 nM against 66% of the cell lines evaluated among a total of 1,094 cancer cell lines. Moreover,Verucopeptin displays tissue specificity, such as leukemia, lymphoma, and melanoma, are classified in the lower IC₅₀ groups, while the higher IC₅₀ groups including other cancer types, such as non-small cell lung cancer^[3].
Verucopeptin (10 nM; 1 hour) pretreatment blocks VE-P labeling of ATP6V1G1 but not ATP1V1B2 or ATP6V1D in a competitive binding assay. Verucopeptin shows substantial inhibition of v-ATPase activity and suppresses lysosomal acidification in vitro, as does Baf A1, although to a lesser extent^[3].
Verucopeptin (0-500 nM; 1 hour) exhibits substantial inhibition of p-S6K as well as p-4EBP1 at concentrations of 10-200 nM. Additionally, Verucopeptin attenuates the phosphorylation of most of the tested mTORC1 downstream substrates, including p-4EBP1, pmTOR^S2448, p-mTOR^S2481, p-Rictor, p-ULK1, and p-Grb10, at concentrations ranging from 50 nM to 500 nM^[3].
Verucopeptin (0-335 nM; 24 hour) decreases the HIF-1 protein level in a dose-dependent manner but has no effects on c-Raf in HT1080 cells. However, the known hsp90 inhibitor Tanespimycin (HY-10211) inhibits both HIF-1 and c-Raf expression in cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.