计算溶液所需的质量、体积或浓度。
概述
Verucopeptin is a potent? HIF-1 ( IC 50 =0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels 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
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 IC 50 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 IC 50 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 IC 50 groups, while the higher IC 50 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 inhibits both HIF-1 and c-Raf expression in cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice by subcutaneous injection of SGC7901/VCR cellsDosage: 1 mg/kg Administration: Intravenous injection; 1 mg/kg; twice daily; 7 days Result: Exhibited profound antitumor efficacy in vivo against MDR tumors.
Form:Solid
IC50& Target:IC50: 0.22 μM (HIF-1),IC50: v-ATPase ATP6V1G subunit
规格
别名
维鲁肽素
规格或纯度
≥98%
英文名称
Verucopeptin
生化机理
Verucopeptin 是一种强效的 HIF-1 抑制剂（IC50=0.22 μM），可降低 HIF-1 靶基因的表达和 HIF-1α 蛋白水平。Verucopeptin 直接靶向 v-ATPase ATP6V1G 亚基，而不是 ATP1V1B2 或 A-A-ATPase，从而强烈抑制 v-ATPase 的活性。
储存条件
干燥,-80℃储存
运输条件
特低温运输
纯度
≥98%
名称和识别符
分子类型
小分子
Smiles
CC[C@@H](C)C[C@H](C)C[C@H](C)/C=C(\C)/[C@@H]1[C@H](CCC(O1)([C@@](C)(C(=O)N[C@H]2[C@@H](OC(=O)CN(C(=O)CNC(=O)CN(C(=O)CN(C(=O)[C@H]3CCCNN3C2=O)O)C)C)C(C)C)O)O)OC
Isomeric SMILES
CC[C@@H](C)C[C@H](C)C[C@H](C)/C=C(\C)/[C@@H]1[C@H](CCC(O1)([C@@](C)(C(=O)N[C@H]2[C@@H](OC(=O)CN(C(=O)CNC(=O)CN(C(=O)CN(C(=O)[C@H]3CCCNN3C2=O)O)C)C)C(C)C)O)O)OC
PubChem CID
分子量
896.08
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?80 °C、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 138067-14-8，分子式为 C43H73N7O13，分子量为 896.08 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）