Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy.
IC50&Target
EC50: 12.2 µM (Ebolavirus)
体外研究
Retro-2 (1 μM; 1-4 hours) induces autophagy in GFP-LC3-expressing HeLa cells and promoted the dramatic cytoplasmic accumulation of large autophagosomes.
Retro-2 (1 μM; 0.5-4 hours) treatment hows an increase over time of the abundance of LC3-II protein in cells.
Retro-2 impairs the trafficking between autophagosomes and lysosomes. Retro-2 abolishes autolysosomes formation.
Retro-2 (20 μM; pretreatment for 30 min) inhibits HeLa cell intoxication by ricin, Shiga-like toxins 1 (Stx1) and 2 (Stx2).
Retro-2 blocked invasion of cells by the intracellular parasite Leishmania, as well as replication of non-enveloped viruses, including polyoma-, papilloma-, and adeno-associated viruses.
Cell Autophagy Assay
Cell Line:
HeLa cells
Concentration:
1 μM
Incubation Time:
1 hour, 2 hours, 4 hours
Result:
Resulted in a large significant increase in the number of small and large vesicles.
Western Blot Analysis
Cell Line:
HeLa cells
Concentration:
1 μM
Incubation Time:
0.5 hour, 2 hours, 4 hours
Result:
Showed an increase over time of the abundance of LC3-II protein in cells.
体内研究
Retro-2 (2-200 mg/kg; i.p; daily; for 21 days) treatment clearly protects from lethal nasal exposure to ricin in mice. 200 mg/kg of Retro-2 fully protects mice against ricin challenge.
Animal Model:
Female Balb/c mice (Pathogen-free 6-week-old) injected with ricin (2 μg/kg)
Dosage:
2 mg/kg, 10 mg/kg, 20 mg/kg, 200 mg/kg
Administration:
Intraperitoneal injection; daily; for 21 days
Result:
Protected mice against ricin challenge.
分子式
C19H16N2Os
分子量
320.41
CAS号
1201652-50-7
运输条件
Room temperature in continental US; may vary elsewhere.