Antileishmanial agent-44 

Antileishmanial agent-44 is a histone deacetylase inhibitor targeting Leishmania donovani Sir2, with an IC₅₀ of 0.652 μM against amastigotes. Antileishmanial agent-44 elevates ROS levels to induce oxidative stress, which causes mitochondrial membrane potential depolarization, cytochrome c release, phosphatidylserine externalization and DNA fragmentation, triggers apoptosis-like cell death, and arrests the cell cycle. Antileishmanial agent-44 upregulates the expression of Th1-type cytokines and NO in macrophages, reshapes host immune responses to eliminate intracellular parasites. Antileishmanial agent-44 inhibits parasites in infected golden hamsters in vivo. Antileishmanial agent-44 can be used for the research of visceral leishmaniasis.

Antileishmanial agent-44 (11ad) potently inhibits Leishmania donovani amastigotes in J774A.1 macrophages, with an IC₅₀ of 0.652 μM, and achieves an inhibition rate of 99% after treatment at 25 μM for 72 h^[1].
Antileishmanial agent-44 exhibits low cytotoxicity against J774A.1 macrophages, with a CC₅₀ of 529.0 μM and a selectivity index of 811.3^[1].
Antileishmanial agent-44 (48 h) regulates host immune responses in Leishmania donovani-infected J774A.1 macrophages by upregulating the Th1 cytokines TNF-α and IFN-γ, and downregulating the Th2 cytokine IL-10^[1].
Antileishmanial agent-44 (10 μM; 24-48 h) induces nitric oxide production in J774A.1 macrophages; after treatment with 10 μM for 24 h and 48 h, 39.1% and 62.4% of the cells exhibit nitric oxide-related fluorescence, respectively^[1].
Antileishmanial agent-44 (10 μM; 60-90 min) potently inhibits the histone deacetylase activity of purified recombinant Leishmania donovani Sir2 protein, reaching an inhibition rate of 77.83% at 10 μM after 60−90 min of incubation^[1].
Antileishmanial agent-44 (10-50 μM; 24-72 h) induces apoptosis-like cell death in Leishmania donovani promastigotes; significant oligonucleosomal DNA fragmentation is observed after treatment with 50 μM for 48 h and 72 h^[1].
Antileishmanial agent-44 (10 μM; 24-48 h) disrupts the cell cycle of Leishmania donovani promastigotes, causing time-dependent accumulation of cells in the sub-G₀/G₁ phase after treatment at 10 μM^[1].
Antileishmanial agent-44 (10 μM; 12-48 h) induces oxidative stress and mitochondrial dysfunction in Leishmania donovani promastigotes, leading to elevated reactive oxygen species (ROS) levels, loss of mitochondrial membrane potential, and time-dependent release of cytochrome c from mitochondria to the cytosol after treatment with 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Antileishmanial agent-44 (11ad) (50 mg/kg; i.p.; daily; 5 days) achieves 88.4% inhibition of splenic amastigote burden in L. donovani-infected golden hamsters^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

444.57

C₃₀H₂₈N₄

CC(C)(C)NC1=C(N=C2N1C(C3=CC=CC=C3C)=C4C(C5=C(C=CC=C5)N4)=C2)C6=CC=CC=C6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ghosh A, et al. Synthesis and Assessment of Imidazo-Fused β-Carbolines as Antileishmanial Agents. ACS Infectious Diseases. 2026;12(6):2124-2135.