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Verucopeptin

CAS No. : 138067-14-8

MCE 站：Verucopeptin

产品活性：Verucopeptin 是一种有效的 HIF-1 (IC₅₀=0.22 μM) 抑制剂，可以降低 HIF-1 靶基因的表达和 HIF-1α 的蛋白水平。通过直接靶向 v-ATPase ATP6V1G 亚基 (但不靶向 ATP1V1B2 或 ATP6V1D)，Verucopeptin 强烈抑制 v-ATPase 活性。Verucopeptin 对耐药性癌细胞表现出抗肿瘤活性，常用作癌症相关研究。

研究领域：Metabolic Enzyme/Protease  |  Membrane Transporter/Ion Channel

作用靶点：HIF/HIF Prolyl-Hydroxylase  |  Proton Pump  |  Endogenous Metabolite

In Vitro: ATP6V1G, a subunit of the vacuolar H⁺-ATPase (v-ATPase).
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.
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.
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.
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.
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.

In Vivo: Verucopeptin (intravenous injection; 1 mg/kg; twice daily; 7 days) substantially represses tumor growth without significant body weight loss or gross signs of toxicity. HE staining indicated that Verucopeptin potently induces cell death ａnd abrogates mTORC1 signaling by dephosphorylation of S6K ａnd 4EBP1.

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