| Identification | Back Directory | [Name]
2,3-Dihydro-2-(5-methyl-2-thienyl)-3-phenyl-4(1H)-quinazolinone | [CAS]
1429192-00-6 | [Synonyms]
Retro-2
RN 1-001
Retro-2 cycl
Retro-2 >=98% (HPLC)
2,3-Dihydro-2-(5-methyl-2-thienyl)-3-phenyl-4(1H)-quinazolinone
4(1H)-Quinazolinone, 2,3-dihydro-2-(5-methyl-2-thienyl)-3-phenyl-
2-(5-methylthiophen-2-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one | [Molecular Formula]
C19H16N2OS | [MDL Number]
MFCD28124399 | [MOL File]
1429192-00-6.mol | [Molecular Weight]
320.41 |
| Hazard Information | Back Directory | [Description]
Retro-2 is a selective inhibitor of retrograde protein trafficking mediated by syntaxin-5 at the interface between the endosome and trans-Golgi network, with no discernable effects on other intracellular trafficking pathways. Retro-2 inhibits ebolavirus infection with an EC50 value of 12.2 μM and reduces ricin-induced toxicity by 2.7-fold when used at a concentration of 20 μM in HeLa cells. Retro-2 also blocks JC polyomavirus, BK polyomavirus, and SV40 infectivity in Vero green monkey kidney epithelial cells in vitro (EC50s = 28.4, 61.2, and 58.6 μM, respectively). In mouse models, Retro-2 improves survival and reduces symptoms following infection with Shiga toxin-producing E. coli when administered at a dose of 100 mg/kg and protects against ricin challenge when administered prophylactically at a dose of 2 mg/kg. | [Uses]
Retro-2 is an inhibitor of Ribosome-Inactivating Proteins (RIPs) as well as a blocker of Leishmania parasitophorous vacuoles (LPV) development. | [Biochem/physiol Actions]
Retro-2 is a non-toxic inhibitor of the endosome-to-Golgi retrograde transport that selectively protect cells from ricin, cholera toxin, and Shiga-like toxins, without affecting compartment morphology, endogenous retrograde cargos, or other trafficking steps. | [in vivo]
Retro-2 cycl (2-50 mg/kg, once daily for 7 days) can significantly protect 90% of newborn mice from lethal EV71 challenge[3]. | Animal Model: | Newborn mice induced by EV71-WT[3] | | Dosage: | 2, 10, 50 mg/kg; daily; 7 days | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Improved the survival rate of infected mice. |
| [storage]
Store at -20°C, protect from light | [References]
[1] MATHIEU E NONNENMACHER. Syntaxin 5-dependent retrograde transport to the trans-Golgi network is required for adeno-associated virus transduction.[J]. Journal of Virology, 2015, 89 3: 1673-1687. DOI: 10.1128/jvi.02520-14
[2] BAHNE STECHMANN. Inhibition of retrograde transport protects mice from lethal ricin challenge.[J]. Cell, 2010, 141 2: 231-242. DOI: 10.1016/j.cell.2010.01.043
[3] OLENA SHTANKO . Retro-2 and its dihydroquinazolinone derivatives inhibit filovirus infection[J]. Antiviral research, 2018, 149: Pages 154-163. DOI: 10.1016/j.antiviral.2017.11.016
[4] CHRISTIAN D S NELSON. A retrograde trafficking inhibitor of ricin and Shiga-like toxins inhibits infection of cells by human and monkey polyomaviruses.[J]. mBio, 2013: e00729-13. DOI: 10.1128/mbio.00729-13
[5] T SECHER. Retrograde Trafficking Inhibitor of Shiga Toxins Reduces Morbidity and Mortality of Mice Infected with Enterohemorrhagic Escherichia coli.[J]. Antimicrobial Agents and Chemotherapy, 2015: 5010-5013. DOI: 10.1128/aac.00455-15 |
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