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Description: PF-06928215 is a novel, potent, high affinity and selective cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 umy. PF-06928215 is a high affinity (KD = 200 nM) active site-targeting, substrate-competitive cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 4.9 uM; in the presence of 1 mM ATP, 0.3 mM GTP, 100 nM 45-bp interferon-stimulatory dsDNA (ISD)). PF-06928215 displays no inhibitory potency against dsDNA-induced IFN-beta expression in cellular cGAS assays, most likely due to limited cell-permeability and/or high levels of cellular ATP and GTP in the reporter cells employed.
References: PLoS One. 2017 Sep 21; 12(9):e0184843.
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