DHQZ 36

DHQZ 36 is a potent inhibitor of retrograde trafficking. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages with an EC50 of 13.63 μM. DHQZ 36 has potent anti-parasite activity[1].

Research Areas >> Infection

EC50: 13.63 μM (Leishmania amazonensis)[1]

With increasing concentrations of DHQZ 36 there is a significant diminution in the size of parasitophorous vacuoles (LPVs), vacuole sizes are reduced by 30% at 50 μM. These parasites also cause a reduction in the number of parasites per macrophage. Significant parasite loss is observed with as low as 5 μM after treatment with DHQZ 36. Parasites are unable to recover growth when treated with DHQZ 36 at concentrations at or above 12.5 μM[1]. DHQZ 36 causes over 40% reduction in secreted of parasite proteins. DHQZ 36 causes a reversal in Leishmania induced suppression of IL-6 release by infected cells after LPS activation[1].

[1]. Craig E, et al. Structurally optimized analogs of the retrograde trafficking inhibitor Retro-2cycl limit Leishmania infections. PLoS Negl Trop Dis. 2017 May 15;11(5):e0005556.