GT-02216

GT-02216 binds to GCase protein in a dose-dependent manner at both acidic pH 5.0 (K_D = 54.2 μM) and neutral pH 7.4 (K_D = 55 μM) with similar binding affinity^[1].
GT-02216 (12.5 μM, 4 days) shows significant enhancement of GCase activity in mutant GBA1 fibroblasts as well as in GBA1^WT(XY) fibroblasts, except for the GBA1^{L444P/L444P(I)β} cell line, which shows undetectable GCase activity^[1].
GT-02216 (1.56-25 μM, 10 days) decreases the accumulation of HexCer in both GBA1^{L444P/L444P(I)α} and GBA1^WT(XX) cells in a dose-dependent manner^[1].
GT-02216 (4 days) rescues GCase activity in a dose-dependent manner in Tau-GBA1^{L444P/L444P(I)α} fibroblasts and elicites a dose-dependent increase in GCase activity also in Tau-GBA1^WT(XX) fibroblasts^[1].
GT-02216 (1.56-25 μM, 4 days) can reduce tau accumulation both at basal (no seeds) or in the presence of tau seeds in a dose-dependent manner in tau-GBA1^{L444P/L444P(I)α} and tau-GBA1^WT(XX)fibroblasts^[1].
GT-02216 (12.5 μM, 4 days) reversed the increase in LAMP1-positive DOs in Tau-GBA1^{L444P/L444P(I)α} and Tau-GBA1^WT(XX) fibroblasts after Tau seed treatment^[1].
GT-02216 (0-3 μM, 48 h) effectively rescues cell viability in the TauO-challenged hippocampal neurons, demonstrating its neuroprotective potential against TauO-induced neurotoxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.