PARP1-IN-44
PARP1-IN-44
SKU:QM-0014939
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Product Details
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Description
PARP1-IN-44, an Olaparib 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].
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Molecular Formula
C27H22F2N4O4S
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Molecular Weight
536.55
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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
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Target
Apoptosis; DNA/RNA Synthesis; PARP; Reactive Oxygen Species (ROS) ; STING
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Isoform
PARP1; PARP2; PARP3; PARP7; TNKS1/PARP5A; TNKS2/PARP5B
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Shipping Conditions
Room temperature
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PARP1-IN-44
PARP1-IN-44 is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.