|
Cat.No.
|
Product
|
M.W.
|
Description/Specifity of Inhibitor
|
Solubility Stability
|
ConcentrationRangea)
|
Size
|
|
|
AEBSF-HCl
|
239.7
|
Irreversible inhibitor of Thrombin and other serine proteases. Inhibits by acylation of the active site of the enzyme. Much less toxic than PMSF and DFP.
凝血酶及其他絲氨酸蛋白酶的不可逆抑制劑，將活性位點?；?。比PMSF 和DFP毒性小得多。
|
H2O,Aqueous solutions are stable between pH 5-6
|
0.1 - 2 µM
|
500 mg
1 g
|
|
|
Amastatin-HCl
|
511
|
Non-toxic reversible metallo -protease inhibitor. Inhibits many membrane-bound peptidases which are critical regulators of peptide hormones, e.g. aminopeptidase A and M, but not aminopeptidase B. Inhibits also leucine minopeptidase
金屬蛋白酶可逆的抑制劑，無毒?？梢种圃S多肽激素類的膜結(jié)合肽，如氨基肽酶A和M（但不包括氨基肽酶B），也抑制亮氨酸氨基肽酶。
|
Ethanol
0.5 % AcOH
|
1 - 100 µM
|
1 mg
|
|
|
ε-Aminocaproic acid
|
131.2
|
Highly active inhibitor of fibrinolysin and chymotrypsin.
溶纖維蛋白酶和胰凝乳蛋白酶的高活性抑制劑。
|
H2O
|
1 - 20 µM
|
100 g
|
|
|
α-Antichymot-ypsin from human plasma
|
68000
|
Glycoprotein that inhibits chymotrypsin-like proteases (above all human neutrophil cathepsin G) by forming stable complexes. Acute phase protein; concentration in plasma increases after events like inflammation or tissue damage
通過形成穩(wěn)定的復(fù)合物抑制胰凝乳蛋白酶類（包括所有嗜中性人組織蛋白酶G）的糖蛋白。急性時相蛋白；在發(fā)炎或組織損傷時在血漿中濃度會增加。
|
Aqueous buffers
|
Used at equimolar concentration
|
1 mg
|
|
|
Antipain-HCL
|
678.2
|
Reversible inhibitor of serine and cysteine proteases. Inhibits papain and trypsin more specificly than leupeptin. Plasmin is inhibited only slightly. Also involved in inhibition of RNA synthesis
絲氨酸和半胱氨酸蛋白酶可逆的抑制劑。比亮抑酶肽抑制木瓜蛋白酶和胰蛋白酶的專一性更高。
|
H2O
Methanol DMSO
|
1 - 100 µM
|
5 mg
25 mg
|
|
|
Antithrombin III from human plasma
|
ca. 60000
|
Glycoprotein that plays a major role in controlling serine proteases in the blood clotting cascade. Inactivates above all thrombin by forming an extremely stable complex, an effect which is enhanced by heparin. Inhibits also other proteases of the coagulation cascade like plasmin, kallikrein, factor IXa, Xa, XIa & XIIa.
主要在血液凝結(jié)中控制絲氨酸蛋白酶的糖蛋白。通過形成非常穩(wěn)定的復(fù)合物抑制凝血酶的活性，可增強肝素鈉的作用。也可抑制其他凝集類的蛋白酶，如纖維蛋白溶酶、激肽釋放酶、IXa, Xa, XIa 和 XIIa因子。
|
H2O
|
Used at equimolar concentrations
|
1 mg
|
|
|
α1-Antitrypsin from human plasma α1-proteinase inhibitor
|
ca.
53000
|
Glycoprotein that is mainly involved in the control of neutrophil elastase activity. Inhibits also most of other mammalian serine proteases but at a lower rate. Blocks the action of target enzymes by binding nearly irreversibly to their active site.
主要控制嗜中性酯酶活性的糖蛋白。也抑制大多數(shù)其他哺乳動物絲氨酸蛋白酶但速率低。與附近目標(biāo)酶的活性位點不可逆的結(jié)合。
|
H2O
Aqueous buffers
|
Used at equimolar concentra tions
|
5 mg
|
|
|
Aprotinin (Trypsin inhibitor from bovine lung)
|
ca.
6500
|
Basic single-chain polypeptide that inhibits numerous serine proteases by binding to the active site of the enzyme, form ing tight complexes. It inhibits above all plasmin, kallikrein, trypsin, chymotrypsin and urokinase but not carboxypeptidase A and B, papain, pepsin, subtilisin, thrombin and factor X. Used in cell culture to prevent proteolytic damage to cells and to extend lifetime of cells.
基本的單鏈多肽，通過與酶的活性位點緊密結(jié)合形成復(fù)合物，抑制大多數(shù)的絲氨酸蛋白酶。抑制所有的纖維蛋白溶酶、激肽釋放酶、胰蛋白酶、胰凝乳蛋白酶和尿激酶，但不包括羧肽酶A和B、木瓜蛋白酶、胃蛋白酶、枯草菌蛋白酶、凝血酶和X因子。用于細(xì)胞培養(yǎng)中防止細(xì)胞蛋白的水解并延長細(xì)胞壽命。
|
H2O,Aqueous buffers. Sterile iltered solutions at pH 5-8 are stable for several months. Denatures at pH > 12
|
In cell culture: 0.01 - 3 µg/mL; in other applications: 10 - 250 µg/mL
|
10 mg
25 mg
100 mg
|
|
|
Arphamenine A
|
387.4
|
Inhibitor of the metallo-protease Aminopeptidase B
金屬蛋白酶氨基肽酶B的抑制劑
|
H2O, MeOH
|
IC50:
0.006 µg/mL
|
5mg
|
|
|
Arphamenine B
|
403.4
|
Inhibitor of the metallo-protease Aminopeptidase B
金屬蛋白酶氨基肽酶B的抑制劑
|
H2O, MeOH
|
IC50:
0.002 µg/mL
|
5 mg
|
|
|
Benzamidine-HCl
|
174.6
|
Potent inhibitor of thrombin and trypsin
凝血酶和胰蛋白酶有效的抑制劑
|
H2O
|
0.1 - 50 µM
|
5 g
25 g
|
|
|
Bestatin-HCl
|
344.8
|
Metalloprotease inhibitor with multi-pharmacological functions. Inhibits cell surface aminopeptidases (notably B) and leucine aminopeptidase. Inhibitor of leukotriene A4 hydrolase and of enkephalin degradation in cell preparations from brain. Has anticarcinogenic and immunomodulating properties.
多種藥理學(xué)功能的金屬蛋白酶抑制劑。抑制細(xì)胞表面氨基肽酶（特別是B）和亮氨酸氨基肽酶。白三烯A4水解酶和腦細(xì)胞降解產(chǎn)生的腦啡肽的抑制劑。有抗癌和免疫調(diào)節(jié)功能。
|
Methanol
(5 mg/mL)
|
1 - 150 µM
Mitogenic effects at nmolar concentrations
|
5 mg
|
|
|
CA-074
|
383.4
|
Inhibitor of Cathepsin B
組織蛋白酶B的抑制劑
|
DMSO
|
0.01 - 1 µM
|
5 mg
|
|
|
CA-074-Me
|
397.5
|
Proinhibitor for intracellular Cathepsin B. Membrane-permeable analog of CA-074
細(xì)胞內(nèi)組織蛋白酶B的抑制劑前體。與CA-074膜滲透性類似。
|
DMSO
|
1 µM
|
5 mg
|
|
|
Calpain Inhibitor I
|
367.2
|
Tripeptide aldehyde. Specific inhibitor of the Ca2+-dependent cysteine protease calpain I and of cathepsin B and L.
三肽醛。Ca2+依賴性半胱氨酸蛋白酶鈣蛋白酶I和組織蛋白酶B 和 L專屬抑制劑
|
Ethanol,
Methanol, DMF, DMSO (10mg/mL)
|
1 - 50 µM
|
25 mg
|
|
|
Calpain Inhibitor II
|
385.2
|
Tripeptide aldehyde. Specific inhibitor of the Ca2+-dependent cysteine protease calpain II and of cathepsin B and L.
三肽醛。Ca2+依賴性半胱氨酸蛋白酶鈣蛋白酶II和組織蛋白酶B 和 L專屬抑制劑
|
Ethanol, Methanol, DMF, DMSO(10 mg/mL)
|
1 -50 µM
|
25 mg
|
|
|
Cathepsin Inhibitor Z-Phe-Gly-NHO- Bz-pMe
|
489.5
|
Specific inhibitor of Cathepsin B/L/S and Papain
組織蛋白酶B/L/S和木瓜蛋白酶的專屬抑制劑
|
DMSO, EtOH, Acetonitrile
|
Ki:
0.15 - 16 µM
|
1 mg
|
|
|
Chymostatin
|
ca.
600
|
Peptide-derived aldehyde (mixture of 3 components). Reversible inhibitor of chymotrypsin-like serine and some cysteine proteases
肽醛（含三種組分）。胰凝乳蛋白酶類絲氨酸和某些半胱氨酸蛋白酶可逆的抑制劑。
|
DMSO
Acetic acid
|
10 - 100 µM
|
5 mg
25 mg
|
|
|
DFP
(Diisopropylfluoro
phosphate)
|
184.2
|
A potent irreversible inhibitor of serine proteases and acetyl choline esterase. Highly toxic!
絲氨酸蛋白酶和乙酰膽堿酯酶高效的不可逆抑制劑。劇毒！
|
Isopropanol; aqueous solutions are unstable
|
10 - 100 µM
|
1 g
|
|
|
Diprotin A
|
341.5
|
Reversible inhibitor of the metallo-protease Dipeptidylaminopeptidase IV
金屬蛋白酶二肽氨基肽酶IV的可逆抑制劑
|
H2O
|
Ki:2.2 µM
|
50 mg
|
|
|
E-64
|
357.4
|
Non-competitive irreversible inhibitor of papain and other cysteine proteases. Forms a thioether bond with the sulfhydryl group in the active center of the enzyme. Useful for active site titration: one mole of E-64 inhibits one mole of protease.
木瓜蛋白酶和其他半胱氨酸蛋白酶非競爭性不可逆的抑制劑。與酶活性中心的巰基形成硫醚鍵。用于活性位點的滴定：1mol的E-64抑制1mol的蛋白酶。
|
H2O, DMSO Mixtures of water and ethanol
|
1 - 10 µM
|
5 mg
25 mg
|
|
|
E-64d (EST)
|
342.4
|
Membrane-permeable analog of E-64c
與E-64c膜滲透性類似
|
DMSO
|
1 µM
|
1 mg
5 mg
|
|
|
Ebelactone A
|
338.5
|
Non-toxic inhibitor for esterases, acylpeptide hydrolase, lipase and N-formylmethionine aminopeptidase.
酯酶、?；乃饷浮⒅久负蚇-甲酰甲硫氨酸氨基肽酶無毒的抑制劑
|
Methanol
(200 mg/mL)
|
1 - 10 µM
|
1 mg
5 mg
|
|
|
Ebelactone B
|
352.5
|
Non-toxic inhibitor for esterase, lipase and N-formyl-methionine aminopeptidase. Inhibits also carboxypeptidase Y-like exopeptidase.
酯酶、脂肪酶和N-甲酰甲硫氨酸氨基肽酶無毒的抑制劑。也抑制羧肽酶Y類外肽酶。
|
Methanol
(200 mg/mL)
|
1 - 10 µM
|
1 mg
5 mg
|
|
|
EDTA-Na2
|
372.3
|
Reversible inhibitor of metalloproteases
金屬蛋白酶的可逆抑制劑
|
H2O (pH 8)
|
1 - 10 µM
|
100 g
1 kg
5 kg
|
|
|
EGTA
|
380.4
|
Inhibits metalloproteases.. Reveals high selectivity for Ca2+ over Mg2+ ions.
Ca2+ over Mg2+ ions.
抑制金屬蛋白酶。對Ca2+ 的選擇性高于 Mg2+。
|
NH4OH, NaOH
|
1 - 10 µM
|
5g
50 g
|
|
|
Elastatinal
|
512.6
|
Inhibitor of Elastase
彈性蛋白酶的抑制劑
|
H2O, MeOH, DMSO
|
Ki: 0.21 µM
(with-Ac-Ala-Ala-Ala-OMe as substrate)
|
5 mg
|
|
|
Leuhistin
|
241.3
|
Inhibitor of Aminopeptidase M
氨基肽酶M的抑制劑
|
H2O, DMSO,
EtOH, MeOH
|
IC50:
0.2 µg/ml
|
5 mg
|
|
|
Leupeptin-hemisulfate
|
475.6
|
Tripeptide aldehyde. Reversible competitive inhibitor of serine and cysteine proteases. Inhibits also phospholipase D and C activation in rat hepatocytes.
三肽醛。絲氨酸和半胱氨酸蛋白酶可逆的競爭性抑制劑。也抑制鼠肝細(xì)胞中磷酸酯酶D和C的活化。
|
H2O Stable for sereval months when stored in aliquots at -20 °C
|
1 - 100 µM
|
10 mg
50 mg
|
|
|
α2-Macroglo-bulin from human plamas
|
725000
|
Glycoprotein composed of 4 identical subunits. Broad-range endoproteinase inhibitor. Inhibits by forming a »trap« around the enzyme allowing only small substrate molecules to enter and to be cleaved by the entrapped protease.
含4個相同亞單位的糖蛋白。主要的內(nèi)蛋白酶抑制劑。由截留酶在酶周圍形成一個只能通過小分子底物的缺口。
|
H2O Stable for several months when stored in aliquots at -20 °C
|
Used at equimolar concentrations
|
1 mg
|
|
|
4-(2-Aminoethyl) -benzenesulfonyl fluoride hydrochloride PEFABLOC® SC
|
239.5
|
Water-soluble and relativly non-toxic irreversible inhibitor ofthrombin and other serine proteases. Inhibits by acylation of the active site of the enzyme.
水溶性的無毒不可逆抑制劑，通過酶活性位點的酰基化抑制制凝血酶和其他絲氨酸蛋白酶。
|
H2O(20 g/100 ml) Stable for several months between pH 5 - 6; limited stability above pH 7.5
|
0.1 - 5 mM in cell culture:
0.1 - 0.25 µM
|
100 mg
500 mg
|
|
|
Pepstatin A
|
685.9
|
Pentapeptide derivative. Reversible inhibitor of aspartic proteases, e.g. pepsin, cathepsin D, chymosin,rennin.
五肽的衍生物?？赡娴囊种铺於彼岬鞍酌?，如胃蛋白酶、組織蛋白酶D、凝乳酶
|
Methanol
(1 mg/mL) DMSO
|
1 - 10 µM
|
5 mg
25 mg
100 mg
|
|
|
Phebestin
|
441.5
|
Inhibitor of Aminopeptidase N.
氨基肽酶N的抑制劑
|
H2O, DMSO, MeOH
|
IC50:
0.18 µg/ml
|
1 mg
|
|
|
PMSF
Phenylmethyl sulfonyl fluoride
|
174.2
|
Irreversibly inhibits serine proteases by sulfonylation of the serine residue in the active site of the protease. Inhibits also papain (reversible by DTT treatment) and acetylcholin-esterase. Does not inhibit metallo-, aspartic- and most cysteine proteases.
通過蛋白酶活性位點絲氨酸殘基的磺?；?，不可逆的抑制絲氨酸蛋白酶。也抑制木瓜蛋白酶（用DTT處理可逆）和乙酰膽堿酯酶。但不抑制金屬蛋白酶、天冬氨酸蛋白酶和大多數(shù)半胱氨酸蛋白酶。
|
Isopropanol, ethanol, methanol. (100 - 200mM) Unstable in aqueous solution
|
0.1 - 1 µM
|
5 g
25 g
100 g
|
|
|
Phosphoramidon
|
587.5
|
Specific inhibitor of thermolysin and neutral endopeptidase-24.11 (ANP Degradation Enzyme). Inhibits also the activity of Endothelin Converting Enzyme, collagenase and metallo-endoproteinases from many microorganisms. Does not inhibit serine, cysteine and aspartic proteases.
嗜熱菌蛋白酶和中性內(nèi)蛋白酶-24.11（ANP降解酶）的專屬抑制劑。也抑制內(nèi)源性內(nèi)皮素轉(zhuǎn)化酶、膠原酶和微生物來源的金屬內(nèi)蛋白酶活性。
|
H2O
(20 mg/mL) DMSO Methanol
|
1 - 100 µM
|
5 mg
|
|
|
TLCK
(1-Chloro-3-tosylamido -7-amino-2-heptanone HCl)
|
369.3
|
Irreversibly inhibits trypsin but not chymotrypsin by alkylating the histidine residue in the active site of the enzyme. Inhibits also some other serine and cysteine proteases like bromelain, ficin and papain. TLCK does not react with zymogens or in active protease-inhibitor complexes.
通過乙酰化酶活性位點剩余的組氨酸，不可逆的抑制胰蛋白酶（但不含胰凝乳蛋白酶）。也抑制其他的絲氨酸和半胱氨酸蛋白酶，如菠蘿蛋白酶、無花果蛋白酶和木瓜蛋白酶。不與酶原或活性蛋白酶抑制劑復(fù)合物反應(yīng)。
|
1 mM HCl, DMSO H2O
(20mg/mL). Aqueous solutions are unstable above pH 7
|
10 - 1000 µM
|
100 mg
250 mg
1 g
|
|
|
TPCK
(1-Chloro-3-tosylamido-4-phenyl-2-butanone)
|
351.8
|
Irreversibly inhibits chymotrypsin but not trypsin by specifically reacting with histidine. Inhibits also other serine and cysteine protease such as bromelain, ficin and papain.
通過與組氨酸專一性反應(yīng)，不可逆的抑制胰凝乳蛋白酶（但不含胰蛋白酶）。也抑制其他的絲氨酸和半胱氨酸蛋白酶，如菠蘿蛋白酶、無花果蛋白酶和木瓜蛋白酶。
|
Ethanol (20 mg/mL) sparingly soluble in water; unstable at alkaline pH
|
10 - 1000 µM
|
250 mg
1 g
|
|
|
Trypsin inhibitor from egg white
(Ovomucoid)
|
ca. 28000
|
Monomeric Glycoprotein. Inhibits bovine (but not human) trypsin in a 1:1 molar ratio. Inhibition is reversible and pH dependant.
單體糖蛋白，1：1的濃度可逆的抑制牛（非人）胰蛋白酶，并與pH有關(guān)。
|
H2O,1mM HCl(1mg/mL) Very stable between pH 3 - 7 against heat and 9 M urea. Unstable at alkaline pH
|
Used at equimolar concentrations
(10-100 µg/ml)
|
100 mg
|
|
|
Trypsin inhibitor from soybean
|
ca. 22000
|
Monomeric protein. Reversible serine protease inhibitor. Inhibits trypsin, factor Xa, plasmin and plasma kallikrein, but not tissue kallikrein.
單體蛋白，絲氨酸蛋白酶的可逆抑制劑。抑制胰蛋白酶、因子Xa、血纖維蛋白溶解酶和血漿激肽釋放酶（非組織激肽釋放酶）
|
H2O(1mg/mL) Sensitive to heat and high pH
|
Used at equimolar concentrations (10-100 µg/ml)
|
50 mg
|