Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome[1]. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II[2]. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors[3]. 20S proteasome[1].Topoisomerase I and II[2].
References:
[1]. Isoe T, et al. Inhibition of different steps of the ubiquitin system by CDDP and aclarubicin. Biochim Biophys Acta. 1992 Sep 15;1117(2):131-5. [2]. Hajji N, et al. Induction of genotoxic and cytotoxic damage by aclarubicin, a dual topoisomerase inhibitor. Mutat Res. 2005 May 2;583(1):26-35. [3]. Iihoshi H, et al. Aclarubicin, an anthracycline anti-cancer drug, fluorescently contrasts mitochondria and reduces the oxygen consumption rate in living human cells. Toxicol Lett. 2017 Aug 5;277:109-114.
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) 是一种荧光分子，是第一个发现对 20S 蛋白酶体 (20S proteasome) 的CTRL (糜凝乳蛋白酶样) 活性具有离散特异性的非肽性抑制剂。同时也是 拓扑异构酶 I 和 II (topoisomerase I and II) 的双抑制剂。是一种有效治疗血癌和实体肿瘤的蒽环类化疗药物。