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AdipoGen Dapansutrile

Supplier: AdipoGen AGCR13535M250
Chemical. CAS 54863-37-5. Formula C4H7NO2S. MW 133.2. Dapansutrile is a potent, selective and orally active inhibitor of the NLRP3 inflammasome. It directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 adenosine triphosphatase ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly interaction between NLRP3, Asc and caspase-1 and activation. Dapansutrile is an anti-inflammatory agent by inhibiting the release of inflammatory signals such as IL-1β and IL-18. However, it does not impact the mRNA levels of the NLRP3, ASC, caspase-1, IL-1β and IL-18 genes. In vitro, nanomolar concentrations of Dapansutrile reduce IL-1β and IL-18 release following canonical and noncanonical NLRP3 inflammasome activation. Dapansutrile is selective for NLRP3 over NLRP4 and AIM2 inflammasomes at concentrations up to 100 μM. Known other targets of dapansutrile include several phosphorylated kinases such as Src, Fyn, HcK, and STAT3.
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