CA-074 methyl ester (CA-074 Me)

製品コード:S7420 別名:Cathepsin B Inhibitor IV

For research use only.

CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.

CA-074 methyl ester (CA-074 Me)化学構造

CAS No. 147859-80-1

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 23100
JPY 26400
JPY 84500

代表番号: 03-5615-9297|電子メール:[email protected]



Cathepsin B阻害剤の選択性比較


製品説明 CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
Cathepsin B [1]

CA-074Me is able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei, but does not inhibit cathepsin L in the absence of thiols. CA-074Me is converted into CA-074 by intracellular esterasesand is, therefore, able to inhibit cathepsin B in GSH-depleted HL-60 cell. It is suggested that CA-074 rather than CA-074Me should be used to selectively inhibit cathespsin B within living cells[1]. Myotube size and number and induced levels of fusion-related creatine phosphokinase activity and myosin heavy-chain protein are reduced from 30 to 50% in CA074Me-treated myoblasts. These reductions are also dose related. Micromolar concentrations of CA074Me inhibit catB activity in differentiating myoblasts[2].

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-10A neoT NWT3[oRoTnWwY4Tpc44h[XO|YYm= M4Tl[FIhcHK| MkDmTY5pcWKrdHnvckBw\iClYYTo[ZB{cW5iQjDpckBpfW2jbjDNR2YuOTCDIH7lc3Qh[2WubIOgZZN{\XO|ZXSgZZMheHKxdHXvcJl{cXNib3[g[Zh1emGlZXzseYxieiCvZX3idoFv\SCkeTDt[YF{fXKrbneg[IVkemWjc3WgbY4hcW62cnHj[YxtfWyjcjDk[Ydz[WSjdHnvckBw\iCGUT3jc4xt[WenbjC0JIF1KDVyIIXNJIlv[3WkYYTl[EBnd3JiMjDodpMh\m:ubH;3[YQh[nliRGGtZ49tdGGpZX6gZYRlcXSrb36gcYVie3W{ZXSg[o9zKDJiaILzMi=> NHrmSpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWwN|AzPCd-Mkm1NFMxOjR:L3G+
体内試験 Administration of CA074Me to the London APP mice results in significant improvement in memory deficit, reduces amyloid plaque load in brain, reduces levels of Aβ40 and Aβ42 in brain, and reduces C-terminal β-secretase fragment (CTFβ) derived from APP by β-secretase when compared with untreated control animals. It has no effect on any of these parameters in mice expressing the Swe mutant β-secretase site of APP (in Swedish/London APP mice). In vivo icv administration of CA074Me to normal guinea pigs results in substantial reduction of brain Aβ levels and inhibits β-secretase activity[3].


  • 細胞株:HL-60 cells
  • 濃度: 100 μM
  • 反応時間:2 h
  • 実験の流れ:HL-60 cells are pre-treated for 24 h with 200 μM BSO followed by 60 min with 1 mM DEM. Thereafter, the cells(1×106/ml) are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO, 200 μM BSO and 1 mM DEM at 37°C. Control cultures are treated with 1% DMSO alone or with 100 μM Z-FA-DMK in the presence of 200 μM BSO and 1 mM DEM. Untreated HL-60 cells are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO at 37°C. Untreated control cultures are incubated with 1% DMSO alone or with 100 μM Z-FA-DMK. After 2 h incubation, cells are washed three times with PBS/1% glucose and lysed in 100 mM citrate, pH 5.0, 2% Chaps (106 cells/100 μl). Subsequently, the lysate is centrifuged and the clarified supernatant used to assay for proteolytic activity.
  • 動物モデル:London APP mice
  • 投薬量:1 mg/ml
  • 投与方法:An ALZET osmotic minipump was implanted subcutaneously in the midscapular area of the back of each animal. A catheter was connected to the osmotic minipump and inserted into the lateral ventricle of the brain (icv).

溶解度 (25°C)



分子量 397.47


CAS No. 147859-80-1
Storage 3年 -20°C
2年 -80°C in solvent



mg/kg g μL


% DMSO % % Tween 80 % ddH2O


投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。



質量 濃度 体積 分子量



Handling Instructions


* 必須

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