Apcin is an inhibitor of the anaphase-promoting complex/cyclosome (APC/C). It acts by blocking mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe.
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名称 | Apcin |
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Iupac 化学名称 | 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl (2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl)carbamate InChi Key: ZEXHXVOGJFGTRX-UHFFFAOYSA-N |
同义词 | Apcin; |
英文同义词 | Apcin; |
分子式 | C13H14Cl3N7O4 |
分子量 | 438.65 |
Smile | CC1=NC=C([N+]([O-])=O)N1CCOC(NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)=O |
InChiKey | ZEXHXVOGJFGTRX-UHFFFAOYSA-N |
InChi | InChI=1S/C13H14Cl3N7O4/c1-8-19-7-9(23(25)26)22(8)5-6-27-12(24)21-10(13(14,15)16)20-11-17-3-2-4-18-11/h2-4,7,10H,5-6H2,1H3,(H,21,24)(H,17,18,20) |
Cas号 | 300815-04-7 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 可溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
海关编码 |
Targets | |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Wu F, Dai X, Gan W, Wan L, Li M, Mitsiades N, Wei W, Ding Q, Zhang J. Prostate cancer-associated mutation in SPOP impairs its ability to target Cdc20 for poly-ubiquitination and degradation. Cancer Lett. 2017 Jan 28;385:207-214. doi: 10.1016/j.canlet.2016.10.021. Epub 2016 Oct 22. PubMed PMID: 27780719; PubMed Central PMCID: PMC5148662.
2: Lub S, Maes A, Maes K, De Veirman K, De Bruyne E, Menu E, Fostier K, Kassambara A, Moreaux J, Hose D, Leleu X, King RW, Vanderkerken K, Van Valckenborgh E. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells. Oncotarget. 2016 Jan 26;7(4):4062-76. doi: 10.18632/oncotarget.6768. PubMed PMID: 26716651; PubMed Central PMCID: PMC4826190.
3: de Lange J, Faramarz A, Oostra AB, de Menezes RX, van der Meulen IH, Rooimans MA, Rockx DA, Brakenhoff RH, van Beusechem VW, King RW, de Winter JP, Wolthuis RM. Defective sister chromatid cohesion is synthetically lethal with impaired APC/C function. Nat Commun. 2015 Oct 1;6:8399. doi: 10.1038/ncomms9399. PubMed PMID: 26423134; PubMed Central PMCID: PMC4600715.
4: Kawatani M, Osada H. [Chemical biology and novel molecular-targeted agents in cancer therapy]. Nihon Rinsho. 2015 Aug;73(8):1273-80. Review. Japanese. PubMed PMID: 26281678.
5: Wang L, Zhang J, Wan L, Zhou X, Wang Z, Wei W. Targeting Cdc20 as a novel cancer therapeutic strategy. Pharmacol Ther. 2015 Jul;151:141-51. doi: 10.1016/j.pharmthera.2015.04.002. Epub 2015 Apr 4. Review. PubMed PMID: 25850036; PubMed Central PMCID: PMC4457591.
6: Sackton KL, Dimova N, Zeng X, Tian W, Zhang M, Sackton TB, Meaders J, Pfaff KL, Sigoillot F, Yu H, Luo X, King RW. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. Nature. 2014 Oct 30;514(7524):646-9. doi: 10.1038/nature13660. Epub 2014 Aug 24. PubMed PMID: 25156254; PubMed Central PMCID: PMC4214887.
7: Puram SV, Kim AH, Bonni A. An old dog learns new tricks: a novel function for Cdc20-APC in dendrite morphogenesis in neurons. Cell Cycle. 2010 Feb 1;9(3):482-5. PubMed PMID: 20195072; PubMed Central PMCID: PMC2853878.
8: Algul O, Kaessler A, Apcin Y, Yilmaz A, Jose J. Comparative studies on conventional and microwave synthesis of some benzimidazole, benzothiazole and indole derivatives and testing on inhibition of hyaluronidase. Molecules. 2008 Mar 27;13(4):736-48. PubMed PMID: 18463575.