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Retro-2 cycl

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Chemical Structure| 1429192-00-6 同义名 : RN 1-001;Retro-2
CAS号 : 1429192-00-6
货号 : A1144862
分子式 : C19H16N2OS
纯度 : 98%+
分子量 : 320.408
MDL号 : MFCD28124399
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(374.52 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 5% DMSO+5% Tween80+30% PEG300+water 2 mg/mL clear

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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.21mL

6.24mL

3.12mL
参考文献

[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