{"id":34320,"date":"2022-09-21T12:32:42","date_gmt":"2022-09-21T04:32:42","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=34320"},"modified":"2025-11-15T16:13:56","modified_gmt":"2025-11-15T08:13:56","slug":"ca-074-me-cas-147859-80-1apexbio-%e8%b2%a8%e8%99%9fa8239","status":"publish","type":"post","link":"http:\/\/biopioneer.com.tw\/?p=34320","title":{"rendered":"CA-074 Me | CAS# 147859-80-1APExBIO \u8ca8\u865fA8239"},"content":{"rendered":"

\u86cb\u767d\u9176(Proteases)\u7cfb\u5217\u5546\u54c1->>CA-074 Me <\/span><\/span><\/span><\/span><\/strong><\/p>\n

APExBIO Technology LLC \u662f\u4e00\u5bb6\u9818\u5148\u7684\u5c0f\u5206\u5b50\u6291\u5236\u5291 (Small Molecule Inhibitors)\/\u6d3b\u5316\u5291(Activators)\u3001\u5316\u5408\u7269\u5eab( Compound Libraries)\u3001\u80dc\u80bd(Peptides)\u3001\u6aa2\u6e2c\u8a66\u5291\u76d2(Assay Kits)\u3001\u87a2\u5149\u6a19\u8a18(Fluorescent Label)\u3001\u9176(Enzymes)\u3001\u4fee\u98fe\u6838\u82f7\u9178(Modified Nucleotides)\u3001mRNA \u5408\u6210\u4ee5\u53ca\u5404\u7a2e\u5206\u5b50\u751f\u7269\u5b78\u5de5\u5177\u7684\u4f9b\u61c9\u5546\u3002APExBIO\u63d0\u4f9b\u5ee3\u6cdb\u7684\u7522\u54c1\u7dda\uff0c\u6db5\u84cb 20 \u591a\u500b\u4e0d\u540c\u7684\u7814\u7a76\u9818\u57df\uff0c\u4f8b\u5982\u764c\u75c7(cancer)\u3001\u514d\u75ab\u5b78(immunology)\u3001\u795e\u7d93\u79d1\u5b78(neurosciences)\u3001\u7d30\u80de\u51cb\u4ea1(apoptosis)\u548c\u8868\u89c0\u907a\u50b3\u5b78(epigenetics)\u7b49\u3002\u516c\u53f8\u7e3d\u90e8\u4f4d\u65bc\u7f8e\u570b\u5fb7\u5dde\u4f11\u58eb\u9813USA (Houston, Texas)\uff0c\u81f4\u529b\u65bc\u670d\u52d9\u5168\u7403\u5ba2\u6236\u3002\u9ad8\u5ea6\u91cd\u8996\u7522\u54c1\u54c1\u8cea\u3002\u6240\u6709\u7522\u54c1\u5747\u9075\u5faa\u56b4\u683c\u7684\u751f\u7522\u6307\u5357\uff0c\u4e26\u9644\u6709\u5206\u6790\u8b49\u66f8\u3001HPLC\u3001\u8cea\u8b5c(Mass Spectrum)\u548cHMNR\u4ee5\u53ca\u9ad4\u5916\u9a57\u8b49(in vitro validation)\u3002 APExBIO\u7522\u54c1\u5df2\u88ab\u300aNature\u300b\u3001\u300aCell\u300b\u548c\u300aScience\u300b\u7b49\u773e\u591a\u9802\u7d1a\u540c\u884c\u8a55\u5be9\u671f\u520a\u5f15\u7528\u3002>>\u66f4\u591aAPExBio\u5546\u54c1<\/span><\/strong><\/em><\/span><\/a><\/p>\n

<\/p>\n

\u86cb\u767d\u9176(Proteases)\u4e5f\u7a31\u70ba\u80bd\u9176(peptidases)\u6216\u86cb\u767d\u6c34\u89e3\u9176(proteolytic enzymes)\uff0c\u7531\u5927\u91cf\u50ac\u5316\u80bd\u9375\u6c34\u89e3(hydrolysis)\u4e26\u96a8\u5f8c\u5c0e\u81f4\u86cb\u767d\u8cea\u5e95\u7269(protein substrates)\u964d\u89e3\u70ba\u6c28\u57fa\u9178(amino acids)\u7684\u9176\u7d44\u6210\u3002\u86cb\u767d\u9176(Proteases)\u8207\u591a\u7a2e\u4eba\u985e\u75be\u75c5\u6709\u95dc\uff0c\u5305\u62ec\u764c\u75c7(cancer)\u3001\u795e\u7d93\u9000\u884c\u6027\u75be\u200b\u200b\u75c5(neurodegenerative disorders)\u3001\u708e\u75c7\u6027\u75be\u75c5(inflammatory diseases)\u548c\u5fc3\u8840\u7ba1\u75be\u75c5(cardiovascular diseases)\u3002\u56e0\u6b64\uff0c\u8a31\u591a\u86cb\u767d\u9176\u6291\u5236\u5291\u3010\u5c0f\u5206\u5b50(small molecules)\u548c\u86cb\u767d\u8cea\u3011\u5df2\u88ab\u9451\u5b9a\u70ba\u963b\u65b7\u86cb\u767d\u9176\u7684\u6d3b\u6027(proteases)\u3002\u86cb\u767d\u9176\u6291\u5236\u5291\u53ef\u4ee5\u6839\u64da\u5b83\u5011\u901a\u904e\u5169\u7a2e\u4e00\u822c\u6a5f\u5236\u6291\u5236\u7684\u86cb\u767d\u9176\u985e\u5225\u5206\u70ba\u4e0d\u540c\u7684\u985e\u578b\uff0c\u5373\u4e0d\u53ef\u9006\u7684\u201c\u6355\u7372(trapping)\u201d\u53cd\u61c9\u548c\u53ef\u9006(reversible)\u7684\u7dca\u5bc6\u7d50\u5408\u53cd\u61c9\u3002\u86cb\u767d\u9176\u6291\u5236\u5291\u5df2\u88ab\u7528\u4f5c\u6cbb\u7642\u86cb\u767d\u9176\u76f8\u95dc\u75be\u75c5\u7684\u8a3a\u65b7\u5291(diagnostic)\u6216\u6cbb\u7642\u5291(therapeutic agents)\u3002<\/p>\n

CA-074 Me | CAS# 147859-80-1APExBIO\u00a0 \u8ca8\u865fA8239<\/span><\/strong><\/span><\/a><\/span><\/p>\n

Product Citation+6<\/p>\n

Cathepsin B inhibitor<\/p>\n

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

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CA-074 Me \u662f\u4e00\u7a2e\u53ef\u900f\u904e\u819c\u7684\u9078\u64c7\u6027\u7d44\u7e54\u86cb\u767d\u9176 B (cathepsin B)\u6291\u5236\u5291\uff0cIC50 \u503c\u70ba 36.3 nM [1, 2]\u3002CA-074 Me \u662f CA-074 \u7684\u7532\u916f\u884d\u751f\u7269(methyl ester derivative)\u3002\u5728\u57f9\u990a\u7684\u4eba\u7259\u9f66\u6210\u7e96\u7dad\u7d30\u80de(human gingival fibroblasts)\u4e2d\uff0cCA-074 Me \u5c0d\u7d44\u7e54\u86cb\u767d\u9176 B (cathepsins B)\u6709 95% \u7684\u6291\u5236\u4f5c\u7528\uff0c\u5c0d\u7d44\u7e54\u86cb\u767d\u9176 B cathepsin B)\u548c L (cathepsin L)\u7684\u806f\u5408\u6d3b\u6027\u6709\u90e8\u5206\u6291\u5236\u4f5c\u7528 (54%)\u3002\u9084\u767c\u73fe CA-074 Me \u5728\u9084\u539f\u689d\u4ef6\u4e0b\u6291\u5236\u7d44\u7e54\u86cb\u767d\u9176 L (cathepsin L)\u3002\u7576\u9176\u8207 1.4 mM DTT \u6216 4.2 mM GSH \u9810\u5b75\u80b2 2 \u5c0f\u6642\u6642\uff0c\u5b83\u6291\u5236\u7d14\u5316\u7684\u4eba\u7d44\u7e54\u86cb\u767d\u9176 L (cathepsin L) \u7684\u6d3b\u6027\u8d85\u904e 90%\u3002\u9664\u6b64\u4e4b\u5916\uff0cCA-074 Me \u5728 1.4 mM DTT \u5b58\u5728\u4e0b\u5b8c\u5168\u6291\u5236\u7d44\u7e54\u86cb\u767d\u9176 B (cathepsin B) [2, 3]\u3002<\/p>\n

    \n
  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<\/a><\/li>\n
  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\u2013349.PMID:31840571<\/a><\/li>\n
  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<\/a><\/li>\n
  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<\/a><\/li>\n
  5. Xu Z, Zhang Y, et al. “Novel half-sandwich iridium O\u02c6C (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<\/a><\/li>\n
  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<\/a><\/li>\n<\/ol>\n

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    \"\"<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n
    Physical Appearance<\/td>\nA solid<\/td>\n<\/tr>\n
    Storage<\/td>\nStore at -20\u00b0C<\/td>\n<\/tr>\n
    M.Wt<\/td>\n397.5<\/td>\n<\/tr>\n
    Cas No.<\/td>\n147859-80-1<\/td>\n<\/tr>\n
    Formula<\/td>\nC19<\/sub>H31<\/sub>N3<\/sub>O6<\/sub><\/td>\n<\/tr>\n
    Solubility<\/td>\ninsoluble in H2O; \u226519.88 mg\/mL in DMSO; \u226551.5 mg\/mL in EtOH with ultrasonic<\/td>\n<\/tr>\n
    Chemical Name<\/td>\nmethyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate<\/td>\n<\/tr>\n
    SDF<\/td>\nDownload SDF<\/a><\/td>\n<\/tr>\n
    Canonical SMILES<\/td>\nCCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC<\/td>\n<\/tr>\n
    Shipping Condition<\/td>\nShip with blue ice, or upon other requests.<\/td>\n<\/tr>\n
    General tips<\/td>\nFor obtaining a higher solubility, please warm the tube at 37\u00b0C 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.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

     <\/p>\n

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     <\/p>\n

    \"\"<\/p>\n\n\n\n\n\n\n\n\n\n\n\n
    \u54c1\u9805<\/td>\nCAS#<\/td>\n#\u8ca8\u865f<\/td>\n\u61c9\u7528<\/td>\n<\/tr>\n
    Z-VAD-FMK \u00a0<\/a><\/td>\nCAS# 187389-52-2<\/td>\n\u8ca8\u865f\u00a0A1902<\/td>\n\n

    Proteases<\/p>\n

    ICE-like proteases<\/td>\n<\/tr>\n

    TAPI-1 \u00a0<\/a><\/td>\nCAS#171235-71-5<\/td>\n\u8ca8\u865f\u00a0B4686<\/td>\n\n

    Proteases<\/p>\n

    TACE\/ADAM17 inhibitor Product Citation+3<\/td>\n<\/tr>\n

    Talabostat mesylate<\/a><\/td>\nCAS# 150080-09-4<\/td>\n\u8ca8\u865fB3941<\/td>\n\n

    Proteases<\/p>\n

    DPP4 \u4e8c\u80bd\u57fa\u80bd\u9176\u7279\u7570\u6027\u6291\u5236\u5291<\/td>\n<\/tr>\n

    Z-IETD-FMK<\/a><\/td>\nCAS# 210344-98-2<\/td>\n\u8ca8\u865fB3232<\/td>\ninhibitor of caspase 8<\/td>\n<\/tr>\n
    Cisplatin<\/td>\nCAS# 15663-27-1<\/td>\n\u8ca8\u865fA8321<\/td>\n\u9ad8\u6548\u3001\u5ee3\u8b5c\u7684\u5316\u7642\u85e5\u7269<\/td>\n<\/tr>\n
    17-DMAG (Alvespimycin) HCl<\/a><\/td>\nCAS#467214-21-7<\/td>\n\u00a0\u8ca8\u865fA2213<\/td>\nHsp90 inhibitor<\/td>\n<\/tr>\n
    CA-074 Me\u00a0<\/a><\/td>\nCAS# 147859-80-1<\/td>\n\u8ca8\u865fA8239<\/td>\nCathepsin B inhibitor<\/td>\n<\/tr>\n
    VX-765<\/a><\/td>\nCAS# 273404-37-8<\/td>\n\u8ca8\u865fA8238<\/td>\nCaspase-1 inhibitor<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n