1. Metabolic Enzyme/Protease
    Membrane Transporter/Ion Channel
  2. HIF/HIF Prolyl-Hydroxylase
    Proton Pump
    Endogenous Metabolite
  3. Verucopeptin

Verucopeptin 

目录号: HY-P2657
产品使用指南

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。

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Custom Peptide Synthesis

Verucopeptin Chemical Structure

Verucopeptin Chemical Structure

CAS No. : 138067-14-8

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Description

Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels[1][2]. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research[3].

IC50 & Target

IC50: 0.22 μM (HIF-1)[2]
IC50: v-ATPase ATP6V1G subunit[3]

In Vitro

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, pmTORS2448, p-mTORS2481, 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].

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[3].

Animal Model: BALB/c nude mice by subcutaneous injection of SGC7901/VCR cells[3]
Dosage: 1 mg/kg
Administration: Intravenous injection; 1 mg/kg; twice daily; 7 days
Result: Exhibited profound antitumor efficacy in vivo against MDR tumors.
Molecular Weight

896.08

Formula

C₄₃H₇₃N₇O₁₃

CAS No.

138067-14-8

Sequence

Leu-{Aaa}-Gly-{Sar}-Gly-{Sar} Lactone:(Leu1-Sar6)

Sequence Shortening

L-{Aaa}-G-{Sar}-G-{Sar} Lactone:(Leu1-Sar6)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

VerucopeptinHIF/HIF Prolyl-HydroxylaseProton PumpEndogenous MetaboliteHypoxia-inducible factorsHIFsHIF-PHCANCERTUMORmTORC1HIF-1αanticancer chemotherapyMDR cancerv-ATPaseATP6V1GMultidrug resistanceSGC7901/VCR cellsInhibitorinhibitorinhibit

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