X5050 (X-5050) is a small molecule that inhibits REST silencing in a RE1-dependent manner, targeted REST degradation.
X5050 reduce REST protein levels in cells at a concentration of the 50-100 μM, leading to a 50% REST reduction.
X5050 upregulated neuronal genes targeted by REST in wild-type neural cells, as well as in human induced pluripotent stem cells derived from a Huntington disease (HD) patient.
X5050 increased the expressions of BDNF and several other REST-regulated genes in the prefrontal cortex of mice with quinolinate-induced striatal lesions.
