蛋白酶(Proteases)系列商品->>CA-074 Me

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蛋白酶(Proteases)也稱為肽酶(peptidases)或蛋白水解酶(proteolytic enzymes)，由大量催化肽鍵水解(hydrolysis)並隨後導致蛋白質底物(protein substrates)降解為氨基酸(amino acids)的酶組成。蛋白酶(Proteases)與多種人類疾病有關，包括癌症(cancer)、神經退行性疾​​病(neurodegenerative disorders)、炎症性疾病(inflammatory diseases)和心血管疾病(cardiovascular diseases)。因此，許多蛋白酶抑制劑【小分子(small molecules)和蛋白質】已被鑑定為阻斷蛋白酶的活性(proteases)。蛋白酶抑制劑可以根據它們通過兩種一般機制抑制的蛋白酶類別分為不同的類型，即不可逆的“捕獲(trapping)”反應和可逆(reversible)的緊密結合反應。蛋白酶抑制劑已被用作治療蛋白酶相關疾病的診斷劑(diagnostic)或治療劑(therapeutic agents)。

CA-074 Me | CAS# 147859-80-1APExBIO  貨號A8239

Product Citation+6

Cathepsin B inhibitor

CA-074 Me is a membrane-permeable and selective inhibitor of cathepsin B with IC50 value of 36.3 nM [1, 2].

CA-074 Me 是一種可透過膜的選擇性組織蛋白酶 B (cathepsin B)抑制劑，IC50 值為 36.3 nM [1, 2]。CA-074 Me 是 CA-074 的甲酯衍生物(methyl ester derivative)。在培養的人牙齦成纖維細胞(human gingival fibroblasts)中，CA-074 Me 對組織蛋白酶 B (cathepsins B)有 95% 的抑制作用，對組織蛋白酶 B cathepsin B)和 L (cathepsin L)的聯合活性有部分抑制作用 (54%)。還發現 CA-074 Me 在還原條件下抑制組織蛋白酶 L (cathepsin L)。當酶與 1.4 mM DTT 或 4.2 mM GSH 預孵育 2 小時時，它抑制純化的人組織蛋白酶 L (cathepsin L) 的活性超過 90%。除此之外，CA-074 Me 在 1.4 mM DTT 存在下完全抑制組織蛋白酶 B (cathepsin B) [2, 3]。

1. Jianhua Wang, Lichun Wang, et al. “Cathepsin B aggravates acute pancreatitis by activating the NLRP3 inflammasome and promoting the caspase-1-induced pyroptosis.” Int Immunopharmacol. 2021 May;94:107496.PMID:33639565
2. Zhi X, Zhang Y, et al. “NLRP3 inflammasome activation by Foot-and-mouth disease virus infection mainly induced by viral RNA and non-structural protein 2B.” RNA Biol. 2020;17(3):335–349.PMID:31840571
3. Zhou H, Du R, et al. “Cannabinoid receptor 2 promotes the intracellular degradation of HMGB1 via the autophagy-lysosome pathway in macrophage.” Int Immunopharmacol. 2020;78:106007.PMID:31806570
4. Chen CH, Bhasin S, et al. “Study of Cathepsin B inhibition in VEGFR TKI treated human renal cell carcinoma xenografts.” Oncogenesis. 2019 Feb 22;8(3):15.PMID:30796200
5. Xu Z, Zhang Y, et al. “Novel half-sandwich iridium OˆC (carbene)-Complexes: In vitro and in vivo tumor growth suppression and pro-apoptosis via ROS-mediated cross-talk between mitochondria and lysosomes.” Cancer Lett. 2019 Apr 10;447:75-85.PMID:30673591
6. Yan X, Li F, et al. “Interleukin-1beta released by microglia initiates the enhanced glutamatergic activity in the spinal dorsal horn during paclitaxel-associated acute pain syndrome.” Glia. 2018 Dec 21.PMID:30578561

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	397.5
Cas No.	147859-80-1
Formula	C19H31N3O6
Solubility	insoluble in H2O; ≥19.88 mg/mL in DMSO; ≥51.5 mg/mL in EtOH with ultrasonic
Chemical Name	methyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate
SDF	Download SDF
Canonical SMILES	CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC
Shipping Condition	Ship with blue ice, or upon other requests.
General tips	For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

 

 

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CA-074 Me	CAS# 147859-80-1	貨號A8239	Cathepsin B inhibitor
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• COA (Certificate Of Analysis)
• HPLC (Retest)
• NMR (Nuclear Magnetic Resonance)
• MSDS (Material Safety Data Sheet)
• Datasheet

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