PARP1-IN-46 

PARP1-IN-46 is a potent PARP-1 inhibitor with an IC₅₀ of 2.4 nM. PARP1-IN-46 demonstrates remarkable anti-proliferative activity in both rat (C6) and human (U87MG) glioma cells. PARP1-IN-46 promotes PARP cleavage, triggers DNA damage, and increases ROS. PARP1-IN-46 effectively inhibits the migration, invasion and colony formation of glioma cells, and ultimately induces cell apoptosis. PARP1-IN-46 can be used to the study of glioma^[1].

PARP1-IN-46 (Compound 5c) (24 h) demonstrates consistent antiproliferative activity in C6, U87MG, Ovcar-3 and A549 with IC₅₀s of 1.34, 1.28, 4.91 and 1.37 μM^[1].
PARP1-IN-46 (24 h-14 d) significantly inhibits the migration, invasion and colony formation of C6 and U87MG cells^[1].
PARP1-IN-46 (24 h) significantly increases the proportion of cells undergoing early and late apoptosis C6 and U87MG cells^[1].
PARP1-IN-46 (24 h) significantly induces PARP protein cleavage, and upregulates the expression of DNA damage marker γ-H2AX, while downregulating the anti-apoptotic protein Bcl-2 in C6 cells^[1].
PARP1-IN-46 (24 h) causes DNA damage and significantly increases the ROS levels in both C6 and U87MG cells^[1].

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

305.28

C₁₈H₁₁NO₄

2505146-00-7

O=C(C(C1=CC(OC)=CC=C12)=C3NC2=O)C4=C(C3=O)C=CC=C4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Pathi VB, et al. Isoquinolinone-Naphthoquinone Hybrids as Potent PARP-1 Inhibitors Induce Apoptosis in Glioma via DNA Damage and ROS Generation. J Med Chem. 2025 Sep 25;68(18):19153-19168.  [Content Brief]