SI-W052 is an orally active, brain-penetrant, and selective small molecule inhibitor that targets mTOR and TEX264. It activates autophagy by inhibiting mTOR phosphorylation, enhances TEX264 expression to promote endoplasmic reticulum renewal, and suppresses the release of LPS-induced inflammatory factors (TNF-α, IL-6). SI-W052 shows potential for research into neuroinflammation associated with Alzheimer's disease (AD).