RA375

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RA375 

RA375 是 RPN13 (26S 蛋白酶体亚基) 抑制剂。RA375 激活 UPR 信号、ROS 产生和凋亡。RA375 的抗肿瘤活性是 RA190的 10 倍。

RA375

RA375 Chemical Structure

规格 价格 是否有货
5 mg ￥3500 询问价格 & 货期
10 mg ￥6000 询问价格 & 货期
50 mg ￥17000 询问价格 & 货期
100 mg ￥26000 询问价格 & 货期

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生物活性

RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead[1].

体内研究
(In Vivo)

RA375 (10 mg/kg, ip) inhibits proteasome function and reduces ovarian tumor burden in mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: RA375 (10 mg/kg, ip) inhibits proteasome function and reduces ovarian tumor burden in mice[1].
Dosage: 10 mg/kg.
Administration: IP for a 5 days on, 2 days off cycle for two weeks.
Result: Reduced ovarian tumor burden in mice.
Animal Model: Female Balb/c mice[1].
Dosage: 5, 10, 20, 40, 60, 100 mg/kg (Pharmacological Analysis).
Administration: IP single dose.
Result: The dose of 40 mg/kg on alternate days for two weeks produced no observable toxicities or weight loss.

分子量

589.00

Formula

C30H25ClN4O7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (212.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6978 mL 8.4890 mL 16.9779 mL
5 mM 0.3396 mL 1.6978 mL 3.3956 mL
10 mM 0.1698 mL 0.8489 mL 1.6978 mL

参考文献

  • [1]. Ravi K Anchoori, et al. Structure-function Analyses of Candidate Small Molecule RPN13 Inhibitors With Antitumor Properties. PLoS One. 2020 Jan 15;15(1):e0227727.

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