MDL/TLR4 interaction inhibitor / L6H21 binds to MD-2 (myeloid differentiation protein-2, Kd=33.3 µM) and blocks its interaction with TLR4 (toll-like receptor 4) in LPS-stimulated cells, inhibiting TNFα and IL-6 production.1 Attenuates disease progression in a high-fat diet (HFD) induced NASH mouse model.2 Inhibits obesity-induced cardiomyopathy and fibrosis.3 Reduces ethanol plus LPS-induced liver injury via inhibition of NLRP3 inflammasome activation.4 Provides cardioprotective effects5 and protects against cognitive impairment and brain pathologies in HFD prediabetic rats6. Cell permeable. Active in vivo.
Biochemicals & reagents
24533-47-9
Wang et al. (2015), MD-2 as the target of a novel small molecule, L6H21, in the attenuation of LPS-induced inflammatory response and sepsis; J. Pharmacol., 172 4391 Zhang et al. (2018), Inhibition of MD1-dependent inflammation attenuates the progression of non-alcoholic fatty liver disease; Cell. Mol. Med., 22 936 Fang et al. (2018), Inhibition of myeloid differentiation factor-2 attenuates obesity-induced cardiomyopathy and fibrosis; Biophys. Acta Mol. Basis Dis., 1864 252 Kong et al. (2019), Chalcone Derivative L6H21 Reduces EtOH + LPS-Induced Liver Injury Through Inhibition of NLRP3 Inflammasome Activation; Alcohol Clin. Exp. Res., 43 1662 Sumneang et al. (2022), Inhibition of myeloid differentiation factor-2 attenuates cardiometabolic impairments via reducing cardiac mitochondrial dysfunction, inflammation, apoptosis and ferroptosis in prediabetic rats; Biophys. Acta Mol. Basis Dis., 1868 166301 Oo et al. (2021), L6H21 protects against cognitive impairment and brain pathologies via toll-like receptor 4-myeloid differentiation factor 2 signalling in prediabetic rats; J. Pharmacol., doi:10.1111/bph.15741 Epub ahead of print
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TARGET: Inflammasome -- PATHWAY: TLR signaling; TNF; Cytokine -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Inflammation; Kidney diseaseHeart disease