PARP1-IN-33 (Example 6) is a PARP1 inhibitor ( IC50: 0.41 nM). PARP1-IN-33 has retinal cytoprotective effect, with an EC 50 of 0.02 nM (inhibition on MTS activity of H 2 O 2 induced human retinal pigment epithelial cell) [1].
In Vitro, PARP1-IN-33 is highly protective against hydrogen peroxide-induced damage to retinal cells[1].
References:
[1]. 김은희, et al. Isoquinolinone derivative, preparation method therefor, and pharmaceutical composition, comprising same as active ingredient, for prevention or treatment of poly(adp-ribose)polymerase-1 (parp-1)-associated disease, WO2021086077, WPO, 2021-05-06.
In Vitro, PARP1-IN-33 is highly protective against hydrogen peroxide-induced damage to retinal cells[1].
References:
[1]. 김은희, et al. Isoquinolinone derivative, preparation method therefor, and pharmaceutical composition, comprising same as active ingredient, for prevention or treatment of poly(adp-ribose)polymerase-1 (parp-1)-associated disease, WO2021086077, WPO, 2021-05-06.