Activators & Inhibitors

HDAC-IN-29 (compound 13b) is a potent pan- HDAC inhibitor with antitumor activity.

Aspochalasin M shows moderate activity on HL-60 cells (IC50=20.0 μ M). Aspochalasin M has research potential in leukemia diseases.

BACE1/2-IN-1 (compound 34) is an effective BACE1 and BACE2 inhibitor with IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 has lower Pgp efflux ratio and improved passive permeability. The metabolic stability of BACE1/2-IN-1 in liver microsomes is decreased.

Aldose reductase-IN-3 (Compound 5) is an effective and moderately selective aldose reductase (AR) inhibitor (IC50=3.99 μ M). Aldose reductase is a molecular target involved in various inflammatory diseases (including sepsis). Aldose reductase-IN-3 has research potential in sepsis.

MAO A/HDAC-IN-1 is an effective monoamine oxidase A (MAO A) and HDAC dual inhibitor, which can be used for glioma research.

hCAIX/XII-IN-3 (compound 6q) is a potent, selective inhibitor of hCAIX and hCAXII. hCAIX/XII-IN-3 shows K i values of >10000, >10000, 66.2, 4.4 nM for hCAI, hCAII, hCAIX and hCAXII, respectively .

Fluconazole (mesylate) is a triazole antifungal drug. Fluconazole (mesylate) can used in the treatment and prevention of superficial and systemic fungal infections

Pyruvate Carboxylase-IN-2 is a natural analog of erianin. Pyruvate Carboxylase-IN-2 (compound 29) is a potent inhibitor of pyruvate carboxylase (PC). In cell lysate-based and cell-based PC activity assays, Pyruvate Carboxylase-IN-2 shows IC 50 s of 0.065 and 0.097 μM, respectively. Pyruvate Carboxylase-IN-2 mediates the anticancer effect in human hepatocellular carcinoma (HCC).

PARP-1/HDAC-IN-1 is an effective dual inhibitor of PARP-1/HDAC6, with IC50 of 68.90 nM and 510 nM respectively. PARP-1/HDAC-IN-1 has anti-cancer, anti-migration and anti-angiogenesis activities.