GSK3186899 是 Cdc2 相关激酶 12 的抑制剂，对 L. donovani 的 EC50 为 1.4 μM。

GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.

GSK3186899 is active in cidal axenic amastigote assay with an EC50 value of 0.1 μM. GSK3186899 shows good selectivity against mammalian THP-1 host cells (EC50 value >50 μM). GSK3186899 exhibits a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is more active using human peripheral blood mononuclear cells as the host cells[1].

In the mouse model of infection, GSK3186899 (25 mg/kg; orally) reduces parasite levels by 99%. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). There are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested[1].

1972617-87-0

C19H28F3N7O3S

491.53

GSK3186899

DMSO:200 mg/mL (406.89 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years