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Pepstatin A
僅限科研使用
Pepstatin A
別名: Pepstatin 中文名稱：抑肽素
Pepstatin A (Pepstatin) 是一種強效的aspartic protease抑制劑, 并可抑制HIV的復(fù)制。Pepstatin A 也是 cathepsins D 和 cathepsins E 的抑制劑。Pepstatin A 通過抑制溶酶體蛋白酶來抑制自噬。
Pepstatin A Chemical Structure
CAS: 26305-03-3
產(chǎn)品質(zhì)控
批次：
純度：
99.76%
99.76
Pepstatin A相關(guān)產(chǎn)品
| 相關(guān)靶點 | HIV-1 capsid HIV-1 caspid | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Limonin Temsavir (BMS-626529) | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 蛋白酶抑制劑庫 泛素化化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| MDA-MB-231 | Function assay | 3 days | Inhibition of secreted cathepsin D in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 3 days under pH 6.6 conditioned media followed by substrate addition measured at 5 mins interval for , IC50=0.0001μM. | 29087712 | |
| MDA-MB-231 | Function assay | 3 days | Inhibition of secreted cathepsin E in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 3 days under pH 6.6 conditioned media followed by substrate addition measured at 5 mins interval for , IC50=0.0001μM. | 29087712 | |
| MDA-MB-231 | Function assay | 4 hrs | Inhibition of cathepsin D in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent substrate addition measured at 30 secs interval for 30 mins , IC50=0.1μM. | 29087712 | |
| MDA-MB-231 | Function assay | 4 hrs | Inhibition of cathepsin E in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent substrate addition measured at 30 secs interval for 30 mins , IC50=0.1μM. | 29087712 | |
| MDA-MB-231 | Function assay | 4 hrs | Inhibition of cathepsin D in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent 10 mins trypsinization prior to substrate addition measured , IC50=1μM. | 29087712 | |
| MDA-MB-231 | Function assay | 4 hrs | Inhibition of cathepsin E in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent 10 mins trypsinization prior to substrate addition measured , IC50=1μM. | 29087712 | |
| MCF7 | Function assay | 1 hr | Inhibition of cathepsin D in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay, IC50=5μM. | 19715320 | |
| MCF7 | Function assay | 1 hr | Inhibition of cathepsin E in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay, IC50=5μM. | 19715320 | |
| MCF7 | Function assay | Inhibition of cathepsin D in human MCF7 cells by fluorescence assay, IC50=0.005μM. | 19715320 | ||
| MCF7 | Function assay | Inhibition of cathepsin E in human MCF7 cells by fluorescence assay, IC50=0.005μM. | 19715320 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Pepstatin A (Pepstatin) 是一種強效的aspartic protease抑制劑, 并可抑制HIV的復(fù)制。Pepstatin A 也是 cathepsins D 和 cathepsins E 的抑制劑。Pepstatin A 通過抑制溶酶體蛋白酶來抑制自噬。 | |||
|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Pepstatin A對天冬氨酸蛋白酶比如蛋白質(zhì)，組織蛋白酶D和E表現(xiàn)出有效的抑制作用。在HIV感染的H9細胞中，pepstatin A抑制部分細胞內(nèi)HIV gag蛋白質(zhì)的合成，而對HIV感染的細胞沒有顯著毒性。[1] Pepstatin A通過阻斷ERK信號并抑制NFATc1的表達抑制破骨細胞的增殖。[2] |
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|---|---|---|---|---|
化學(xué)信息&溶解度
| 分子量 | 685.89 | 分子式 | C34H63N5O9 |
| CAS號 | 26305-03-3 | SDF | Download Pepstatin A SDF |
| Smiles | CC(C)CC(C(CC(=O)O)O)NC(=O)C(C)NC(=O)CC(C(CC(C)C)NC(=O)C(C(C)C)NC(=O)C(C(C)C)NC(=O)CC(C)C)O | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 50 mg/mL ( (72.89 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 3 mg/mL (4.37 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 1:
Do you have recommended in-vivo solvent for S7381 please?
回答：
S7381 could be dissolved in 5%DMSO+40%PEG300+5%tween-80+ddH2O up to 2mg/ml.
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