E-64

製品コードS7379 バッチS737909

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₂₇N₅O₅

分子量

357.41

CAS No.

66701-25-5

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

71 mg/mL (198.65 mM)

Water (warmed with 50ºC water bath)

20 mg/mL (55.95 mM)

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	E-64は不可逆的かつ選択的なシステインプロテアーゼ阻害剤であり、パパイン、カルパイン、カテプシンBおよびHも阻害しますが、セリンプロテアーゼやアスパラギン酸プロテアーゼは阻害しません。パパインに対するIC50は9 nMです。E-64はフィラリア寄生虫に酸化的ストレスとアポトーシスを誘発します。
in vitro	E-64 rapidly inhibits the activities of the cysteine proteinases cathepsins B, H and L and papain, while has no effect on the serine proteinases or the metalloproteinases. This compound, as a specific inhibitor os cysteine proteases, effectively blocks in vitro ovarian cancer cell invasion. In addition, it also shows antiparasitic activity against Giardia lamblia excystation in vitro. The chemical improves the preimplantation development of bovine somatic cell nuclear transfer embryos, which indicates another important implication of E-64.
in vivo	E-64 induces a marked decrease in the number of spontaneous metastasis in M5076 tumor bearing mice, while has no effect on the formation of experimental metastasis. This compound also shows antiparasitic activity against Giardia lamblia excystation in infected mice.

製品説明

E-64は不可逆的かつ選択的なシステインプロテアーゼ阻害剤であり、パパイン、カルパイン、カテプシンBおよびHも阻害しますが、セリンプロテアーゼやアスパラギン酸プロテアーゼは阻害しません。パパインに対するIC50は9 nMです。E-64はフィラリア寄生虫に酸化的ストレスとアポトーシスを誘発します。

in vitro

E-64 rapidly inhibits the activities of the cysteine proteinases cathepsins B, H and L and papain, while has no effect on the serine proteinases or the metalloproteinases.

This compound, as a specific inhibitor os cysteine proteases, effectively blocks in vitro ovarian cancer cell invasion.

In addition, it also shows antiparasitic activity against Giardia lamblia excystation in vitro.

The chemical improves the preimplantation development of bovine somatic cell nuclear transfer embryos, which indicates another important implication of E-64.

in vivo

E-64 induces a marked decrease in the number of spontaneous metastasis in M5076 tumor bearing mice, while has no effect on the formation of experimental metastasis.

This compound also shows antiparasitic activity against Giardia lamblia excystation in infected mice.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	9 nM
	反応時間
	実験の流れ
動物実験	動物モデル	M5076 tumor bearing mice
	投薬量	--
	投与方法	i.v.

参考

https://pubmed.ncbi.nlm.nih.gov/10380357/
https://pubmed.ncbi.nlm.nih.gov/7044372/
https://pubmed.ncbi.nlm.nih.gov/1617632/

https://pubmed.ncbi.nlm.nih.gov/19530614/
https://pubmed.ncbi.nlm.nih.gov/24240170/
https://pubmed.ncbi.nlm.nih.gov/7919127/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Integrin beta 1 facilitates non-enveloped hepatitis E virus cell entry through the recycling endosome [ Nat Commun, 2025, 16(1):5403]	PubMed: 40571699
Maintenance of neuronal TDP-43 expression requires axonal lysosome transport [ Elife, 2025, 14RP104057]	PubMed: 40970386
Maintenance of neuronal TDP-43 expression requires axonal lysosome transport [ bioRxiv, 2024, 2024.09.30.615241]	PubMed: 39803527
Acquired semi-squamatization during chemotherapy suggests differentiation as a therapeutic strategy for bladder cancer [ Cancer Cell, 2022, 40(9):1044-1059.e8]	PubMed: 36099882
The Antagonizing Role of Heme in the Antimalarial Function of Artemisinin: Elevating Intracellular Free Heme Negatively Impacts Artemisinin Activity in Plasmodium falciparum [ Molecules, 2022, 27(6)1755]	PubMed: 35335120
A lysosome-targeted DNA nanodevice selectively targets macrophages to attenuate tumours [ Nat Nanotechnol, 2021, 10.1038/s41565-021-00988-z]	PubMed: 34764452
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 [ Cell Chem Biol, 2021, S2451-9456(21)00213-0]	PubMed: 33979649
MMP-2 is a novel histone H3 N-terminal protease necessary for myogenic gene activation [ Epigenetics Chromatin, 2021, 14(1):23]	PubMed: 34001241
Small molecule inhibitor E-64 exhibiting the activity against African swine fever virus pS273R [ Bioorg Med Chem, 2021, 35:116055]	PubMed: 33607487
Evaluation of enzymatic proteoglycan loss and collagen degradation in human articular cartilage using ultrashort echo time-based biomarkers: A feasibility study [ NMR Biomed, 2021, e4664]	PubMed: 34904305

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。