RA190
目录号: PL10725 纯度: ≥99%
CAS No. :1617495-03-0
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中文名称
RA190
中文别名
RA190
英文名称
RA190
英文别名
RA190;RA-190;RA190 hydrochloride;s6851;1-(L-phenylalanyl)-3,5-bis(3,4-dichlorobenzylidene)piperidin-4-one hydrochloride;(3Z,5Z)-1-[(2S)-2-Amino-3-phenylpropanoyl]-3,5-bis[(3,4-dichlorophenyl)methylidene]piperidin-4-one;h
Cas No.
1617495-03-0
分子式
C28H23Cl5N2O2
分子量
596.76
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
RA190是双亚苄基哌啶,通过与泛素受体RPN13的半胱氨酸88共价结合来抑制蛋白酶体功能。
生物活性
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
性状
Solid
IC50 & Target[1][2]
IC50: 0.15 μM (HeLa cell)
体外研究(In Vitro)
RA190 covalently binds to cysteine 88 of ubiquitin receptor RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins. Multiple myeloma (MM) lines, even those resistant to bortezomib, are sensitive to RA190 via endoplasmic reticulum stress-related apoptosis. RA190 stabilizes targets of human papillomavirus (HPV) E6 oncoprotein, and preferentially kills HPV-transformed cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
RA190 distributes to plasma and major organs excepting brain, and inhibits proteasome function in skin and muscle. RA190 administration profoundly reduces growth of multiple myeloma and ovarian cancer xenografts, and oral RA190 treatment retards HPV16 syngeneic mouse tumor growth, without impacting spontaneous HPV-specific CD8 T cell responses. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Anchoori RK, et al. A bis-benzylidine piperidone targeting proteasome ubiquitin receptor RPN13/ADRM1 as a therapy for cancer. Cancer Cell. 2013 Dec 9;24(6):791-805.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (167.57 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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