{"id":40898,"date":"2023-04-08T16:27:42","date_gmt":"2023-04-08T08:27:42","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=40898"},"modified":"2025-09-03T11:57:34","modified_gmt":"2025-09-03T03:57:34","slug":"%e9%9b%b7%e5%b8%95%e9%bb%b4%e7%b4%a0-rapamycin-%e8%87%aa%e5%99%acautophagy-activator-cas53123-88-9-mce%e8%b2%a8%e8%99%9fhy-10219","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=40898","title":{"rendered":"\u96f7\u5e15\u9ef4\u7d20( Rapamycin) | \u81ea\u566c(autophagy ) activator CAS#53123-88-9 MCE\u8ca8\u865fHY-10219"},"content":{"rendered":"

\u96f7\u5e15\u9ef4\u7d20( Rapamycin) | \u81ea\u566c(autophagy ) activator CAS#53123-88-9\u00a0MCE\u8ca8\u865fHY-10219 <\/span><\/a><\/span><\/h4>\n

\u96f7\u5e15\u9ef4\u7d20( Rapamycin) (Sirolimus; AY 22989) \u662f\u4e00\u7a2e\u6709\u6548\u7684\u7279\u7570\u6027 mTOR<\/a><\/b>\u00a0i\u6291\u5236\u5291\uff0c\u5728 HEK293 \u7d30\u80de\u4e2d\u7684 IC50 \u70ba 0.1 nM\u3002 Rapamycin \u8207 FKBP12 \u7d50\u5408\u4f75\u7279\u7570\u6027\u5730\u5145\u7576mTORC1<\/a><\/b> \u7684\u8b8a\u69cb\u6291\u5236\u5291\u3002 Rapamycin \u662f\u4e00\u7a2e\u81ea\u566c(autophagy<\/a>)<\/b>\u6fc0\u6d3b\u5291(activator)\uff0c\u4e00\u7a2e\u514d\u75ab\u6291\u5236\u5291(immunosuppressant)\u3002<\/p>\n

<\/p>\n

\u81ea\u566c(Autophagy )<\/span><\/strong><\/span><\/p>\n

\u81ea\u566c(Autophagy )\u662f\u4e00\u7a2e\u7d30\u80de\u5167\u964d\u89e3\u7cfb\u7d71(intracellular degradation system )\uff0c\u53ef\u5c07\u7d30\u80de\u8cea\u6210\u5206\u8f38\u9001\u5230\u6eb6\u9176\u9ad4(lysosome)\u3002\u81ea\u566c\u4f5c\u7528(Autophagy)\u5ee3\u6cdb\u591a\u7a2e\u751f\u7406(physiologica)\u548c\u75c5\u7406\u751f\u7406(pathophysiological)\u4f5c\u7528\u3002\u4e0d\u540c\u7684\u9078\u64c7\u6027\u81ea\u566c\u5f62\u5f0f(\u00a0autophagy)\u5c0e\u81f4\u7d30\u80de\u5668\u6216\u75c5\u539f\u9ad4\u7684\u7279\u7570\u6027\u964d\u89e3\u3002\u9019\u4e9b\u9078\u64c7\u6027\u9014\u5f91\u5305\u62ec\u81ea\u566c\u7dda\u7c92\u9ad4 (mitophagy)\u3001\u904e\u6c27\u5316\u7269\u9176\u9ad4 (pexophagy)\u3001\u5167\u8cea\u7db2 (reticulophagy \u6216 ER-phagy) \u7684\u964d\u89e3\uff0c\u6838\u91a3\u9ad4 (ribophagy)\u3001\u86cb\u767d\u8cea\u805a\u96c6\u9ad4 (aggrephagy)\u3001\u8102\u6ef4 (lipophagy)\u3001\u80f0\u817a\u7d30\u80de\u5167\u7684\u5206\u6ccc\u9846\u7c92\uff08zymophagy\uff09\u6216\u7d30\u80de\u5167\u75c5\u539f\u9ad4\uff08\u7570\u9ad4\u81ea\u566c\uff09\u3002\u81ea\u566c\u7531\u5e7e\u500b\u9023\u7e8c\u7684\u6b65\u9a5f\u7d44\u6210: \u9694\u96e2(sequestration)\u3001\u904b\u8f38\u5230\u6eb6\u9176\u9ad4(\u00a0lysosomes)\u3001\u964d\u89e3(degradation)\u548c\u964d\u89e3\u7522\u7269\u5229\u7528(utilization of degradation products)\uff0c\u6bcf\u4e00\u6b65\u90fd\u53ef\u80fd\u767c\u63ee\u4e0d\u540c\u7684\u4f5c\u7528\u3002\u81ea\u566c\u4fe1\u865f\u8f49\u5c0e(Autophagy signal transduction)\u4e3b\u8981\u53d7\u81ea\u566c\u76f8\u95dc\u8abf\u63a7\u57fa\u56e0\/\u86cb\u767d\u8cea\uff0cAtgs\u3002 ATGs \u63ed\u793a\u4e86\u81ea\u566c\u9ad4\u5f62\u6210\u7684\u5927\u90e8\u5206\u6a5f\u5236\u3002\u6b64\u5916\uff0c\u4e0d\u540c\u7684\u975e ATG\u86cb\u767d\u8cea\u53c3\u8207\u81ea\u566c\u7684\u8abf\u7bc0\u548c\u904e\u7a0b\uff0c\u4f8b\u5982 mTOR\u3001AMPK\u3001AKT\u3001AMBRA1\u3001BCL2\u3001DFCP1 \u6216 VPS34\u3002\u81ea\u566c(Autophagy )\u53ca\u5176\u5931\u8abf\u8207\u4e0d\u540c\u7684\u4eba\u985e\u75be\u75c5\u6216\u904e\u7a0b\u6709\u95dc\uff0c\u4f8b\u5982\u764c\u75c7(cancer)\u3001\u795e\u7d93\u8b8a\u6027(neurodegeneration)\u3001\u514d\u75ab\u529b(immunity)\u6216\u8870\u8001(aging)\u3002\u8a31\u591a\u85e5\u7269\u548c\u5929\u7136\u7522\u7269\u90fd\u53c3\u8207\u81ea\u566c\u8abf\u7bc0(autophagy modulation)\uff0c\u7121\u8ad6\u662f\u901a\u904e\u591a\u7a2e\u4fe1\u865f\u901a\u8def\u8a98\u5c0e\u6216\u6291\u5236\u7d30\u80de\u81ea\u566c\u3002\u6b64\u5916\uff0c\u4e00\u4e9b\u6cbb\u7642\u7cd6\u5c3f\u75c5\u7684\u81e8\u5e8a\u85e5\u7269\u548c\u5316\u5408\u7269\u4e5f\u88ab\u767c\u73fe\u6d89\u53ca\u81ea\u566c\u8abf\u7bc0\u3002<\/p>\n

\u96f7\u5e15\u9ef4\u7d20( Rapamycin) Synonyms: Sirolimus; AY-22989)<\/span><\/strong><\/p>\n

\u96f7\u5e15\u9ef4\u7d20( Rapamycin)\u00a0\uff0812.5-100 nM\uff1b24 \u5c0f\u6642\uff09\u8655\u7406\u5728\u6240\u6709\u6e2c\u8a66\u7684\u7d30\u80de\u682a\uff08A549\u3001SPC-A-1\u300195D \u548c NCI-H446 \u7d30\u80de\uff09\u4e2d\u4ee5\u5291\u91cf\u4f9d\u8cf4\u6027(dose-dependent)\u65b9\u5f0f\u5c0d\u80ba\u764c\u7d30\u80de\u589e\u6b96(cell proliferation )\u7522\u751f\u9069\u5ea6\u6291\u5236\u4f5c\u7528\uff0c\u9054\u5230\u7d04100 nM \u6642\u7d30\u80de\u589e\u6b96\u6e1b\u5c11 30-40%\uff0c\u800c 12.5 nM \u6642\u6e1b\u5c11\u7d04 10%[3]\u3002\u5c07\u80ba\u764c\u7d30\u80de\u682a 95D (Lung cancer cell line 95D cells)\u7d30\u80de\u55ae\u7368\u6216\u806f\u5408\u66b4\u9732\u65bc\u96f7\u5e15\u9ef4\u7d20\uff0810 nM\u300120 nM\uff09\u548c RP-56976\uff081 nM\u300110 nM\uff09\uff08\u96f7\u5e15\u9ef4\u7d20 20 nM + RP-56976 10 nM\uff09\u3002\u55ae\u7368\u66b4\u9732\u65bc\u96f7\u5e15\u9ef4\u7d20( Rapamycin)\u00a0\u6216 RP-56976 24 \u5c0f\u6642\u5f8c\uff0c\u4e0d\u6703\u986f\u8457\u6539\u8b8a ERK1\/2 \u7684\u8868\u9054\u6216\u78f7\u9178\u5316(phosphorylation)\u6c34\u5e73\uff0c\u800c\u96f7\u5e15\u9ef4\u7d20\u8207 RP-56976 \u806f\u5408\u8655\u7406\u7684\u7d30\u80de\u8868\u73fe\u51fa ERK1\/2 \u78f7\u9178\u5316\u6c34\u5e73\u7684\u986f\u8457\u964d\u4f4e[3].<\/p>\n

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<\/p>\n\n\n\n\n\n\n\n\n\n
Molecular Weight<\/th>\n\n
\n

914.17<\/p>\n<\/div>\n<\/td>\n<\/tr>\n

Appearance<\/th>\n\n
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Solid<\/p>\n<\/div>\n<\/td>\n<\/tr>\n

Formula<\/th>\n\n
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C51<\/sub>H79<\/sub>NO13<\/sub><\/p>\n<\/div>\n<\/td>\n<\/tr>\n

CAS No.<\/th>\n\n
SMILES<\/th>\n\n
\n

O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](\/C(C)=C\/C=C\/C=C\/[C@H](C[C@@H](C)C([C@@H]([C@@H](\/C(C)=C\/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](O)CC4)OC)C)=O)=O<\/p>\n<\/div>\n<\/td>\n<\/tr>\n

Structure Classification<\/th>\n\n
\n
Source<\/th>\n\n
\n

bacterium Streptomyces hygroscopicus<\/p>\n<\/div>\n<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

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546 Publications Citing Use of MCE Rapamycin<\/span><\/h5>\n