PARP1-IN-44

PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM) . PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; DNA/RNA Synthesis; PARP; Reactive Oxygen Species (ROS) ; STING

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(NC1(C2)CC2(NS(=O)(C3=CC=C(F)C=C3)=O)C1)C4=CC(CC5=NNC(C6=C5C=CC=C6)=O)=CC=C4F

Molecular Formula

C27H22F2N4O4S

Molecular Weight

536.55

References & Citations

[1]Liu B, et al. Discovery of Bicyclo[1.1.1]pentane-based Olaparib derivatives as novel PARP inhibitors: A dual-action strategy targeting DNA damage and immune activation. Bioorg Chem. 2025 Sep 1;165:108939.