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Pepstatin A

別名: Pepstatin 中文名稱：抑肽素

Pepstatin A (Pepstatin) 是一種強(qiáng)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

Pepstatin A Chemical Structure

CAS: 26305-03-3

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1040.13 現(xiàn)貨
10mg 808.21 現(xiàn)貨
50mg 2270.75 現(xiàn)貨
200mg 5543.31 現(xiàn)貨
1g 22772.3 現(xiàn)貨
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Pepstatin A相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

HIV Protease Signaling Pathways

HIV Protease信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Pepstatin A (Pepstatin) 是一種強(qiáng)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(diǎn)
aspartic protease [1] cathepsins D [2] cathepsins E [2]
體外研究(In Vitro)
體外研究活性

Pepstatin A對(duì)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(xì)胞中，pepstatin A抑制部分細(xì)胞內(nèi)HIV gag蛋白質(zhì)的合成，而對(duì)HIV感染的細(xì)胞沒有顯著毒性。[1]

Pepstatin A通過阻斷ERK信號(hào)并抑制NFATc1的表達(dá)抑制破骨細(xì)胞的增殖。[2]

化學(xué)信息&溶解度

分子量 685.89 分子式

C34H63N5O9
CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 50 mg/mL ( (72.89 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 3 mg/mL (4.37 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(qǐng)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(jìn)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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