|2 -(5-甲基噻吩-2-基)-3-苯基-2- 3-二氢喹唑啉-4(1H)-酮|CsnPharm

CAS No.: 1429192-00-6

Retro-2 cycl Catalog No. CSN23863

Synonyms: RN 1-001

Retro-2 is a specific retrograde trafficking inhibitor of protein toxins.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Retro-2 is a specific retrograde trafficking inhibitor of protein toxins. Retro-2 can selectively block retrograde toxin trafficking at the early endosome-TGN interface and protect cells from ricin and Shiga-like toxins, without affecting compartment morphology, endogenous retrograde cargos, or other trafficking steps, including endocytosis, recycling, degradation, and secretion. Pretreatment with 20μM Retro-2 for 30min could protected HeLa cells from a 4-hour ricin challenge by toxicity reduction of 2.7 fold in HeLa cells, as well as the intoxication by Stx1 and Stx2. Pre-treatment with 20μM Retro-2 inhibited the retrograde transport, but not endocytosis, of STxB to the TGN/Golgi without morphologies of Golgi, ER, of early (EEA1) and recycling endosomes (transferrin receptor [TfR] and Rab11), and of late endosomes/lysosomes (Lamp1) affected. Retro-2 blocked STxB in early endosomes and relocalized Syntaxin 5, but had no effect on endogenous retrograde cargo proteins like CI-MPR and TGN46. Pre-treatment with Retro-2 at dose of 2mg/kg, 10mg/kg, 20mg/kg and 200mg/kg, i.p., for 1h could improve the survival of mice post the ricin toxin challenge in a dose dependent manner^[1]. Retro-2 potently prevented spread of vaccinia virus as well as monkeypox virus by preventing wrapping of virions with an additional double-membrane envelope that enables microtubular transport, exocytosis, and actin polymerization^[2]. Retro-2 elevated the Aβ42-generating activity, by disruption of endosome-to-TGN trafficking ofγ-secretase, both in cultured cells and mice brain, but did not elevate the intrinsic Aβ42-production activity of γ-secretase^[3].
作用机制Retro-2 could block STxB in early endosomes and specifically inhibit retrograde transport to the trans-golgi network.^[1]
动物研究
剂量
Mice: 2 mg/kg - 200 mg/kg^[1] (i.p.)

给药途径
i.p.

毒性数据 (半致死量)
Non-toxicity up to 400mg/kg, i.p., in mice
参考文献

动物研究
剂量	Mice: 2 mg/kg - 200 mg/kg^[1] (i.p.)
给药途径	i.p.
毒性数据 (半致死量)	Non-toxicity up to 400mg/kg, i.p., in mice

[1] Stechmann B, Bai SK, Gobbo E, et al. Inhibition of retrograde transport protects mice from lethal ricin challenge. Cell. 2010;141(2):231-42
[2] Sivan G, Weisberg AS, Americo JL, Moss B. Retrograde Transport from Early Endosomes to the trans-Golgi Network Enables Membrane Wrapping and Egress of Vaccinia Virus Virions. J Virol. 2016;90(19):8891-905
[3] Kanatsu K, Hori Y, Ebinuma I, Chiu YW, Tomita T. Retrograde transport of γ-secretase from endosomes to the trans-Golgi network regulates Aβ42 production. J Neurochem. 2018;147(1):110-123

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1210 mL
- 15.6050 mL
- 31.2100 mL
- 5 mM
- 0.6242 mL
- 3.1210 mL
- 6.2420 mL
- 10 mM
- 0.3121 mL
- 1.5605 mL
- 3.1210 mL

技术信息

CAS号

1429192-00-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H16N2OS

运输

蓝冰

分子量

320.41

别名

RN 1-001

溶解度

DMSO	170.0 mg/mL (530.6 mM)
Water	insoluble

动物实验配方

5% DMSO+5% Tween80+30% PEG300+water

2 mg/mL

clear

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