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 gammaH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-beta and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy[1].
Molekulargewicht:
536.55
Formel:
C27H22F2N4O4S
Target-Kategorie:
Apoptosis,DNA/RNA Synthesis,PARP,Reactive Oxygen Species (ROS),STING
Anwendungsbeschreibung:
MCE Product type: Reference compound
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
