CAS NO: | 108477-18-5 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 414.4 |
Cas No. | 108477-18-5 |
Formula | C19H14N2O7S |
Synonyms | NSC 144303 |
Solubility | ≤15mg/ml in DMSO;1mg/ml in dimethyl formamide |
Chemical Name | tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-4H-thiopyran-4-one, 1,1-dioxide |
Canonical SMILES | O=C(/C(CS(C/1)(=O)=O)=C\C2=CC=C([N+]([O-])=O)C=C2)C1=C/C3=CC=C([N+]([O-])=O)C=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
IC50: ~30 μM
Ubiquitin Isopeptidase Inhibitor I is a ubiquitin isopeptidase inhibitor.
Conjugation or deconjugation of ubiquitin or ubiquitin-like proteins to or from cellular proteins is a multifaceted and universal ways of regulating cellular physiology, controlling the lifetime, localization, and activity of various key proteins.
In vitro: Ubiquitin Isopeptidase Inhibitor I targeted the ubiquitinproteasome system via inhibiting the ubiquitin isopeptidases. Ubiquitin Isopeptidase Inhibitor I could induce a rather unique apoptotic pathway, including a Bcl-2-dependent but apoptosome-independent mitochondrial pathway with upregulation of the BH3-only protein Noxa, stabilization of the inhibitor of apoptosis antagonist Smac, but also the involvement of the death receptor pathway. Moreover, the treatment of Ubiquitin Isopeptidase Inhibitor I to cell extracts obtained from E1A cells did not inhibit the proteolytic activity of the proteasome, whereas MG-132 potently inhibited the cleavage of the LLVY-AMC substrate. In addition, Noxa induction by Ubiquitin Isopeptidase Inhibitor I could be inhibited by the specific RNAi oligos efficiently. When apoptosis was scored, it was found that down-regulation of Noxa was able to inhibit but did not suppress apoptosis and caspase activation in response to Ubiquitin Isopeptidase Inhibitor I treatment [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, Ubiquitin Isopeptidase Inhibitor I is still in the preclinical development stage.
Reference:
[1] E. Aleo, C. J. Henderson, A. Fontanini, et al. Identification of new compounds that trigger apoptosome-independent caspase activation and apoptosis. Cancer Research 66(18), 9235-9244 (2006).