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Thiamet G

CAS No. : 1009816-48-1

MCE 站：Thiamet G

产品活性：Thiamet G 为有效，选择性的 O-GlcNAcase 抑制剂，抑制人 OGA 的 K_i 值为 20 nM。O-GlcNAcase 的作用是从修饰的蛋白质中去除 O-GlcNAc。

研究领域：Autophagy

作用靶点：Autophagy

In Vitro: Thiamet G (1 μM) induces a clear increase in the accumulation of O-GlcNAcylated proteins of ATDC5 cells. O-GlcNAc accumulation induced by Thiamet G also evokes a clear increase in the activity of these MMPs. Thiamet G (1 μM) induces the phosphorylation of JNK, ERK, ａnd p38 but not phosphorylation of Akt. Thiamet G (0.1-10 μM) does not significantly affect the cell viability. Thiamet G decreases phosphorylation of tau ａnd alters the microtubule dynamics.

In Vivo: Thiamet G (500 mg/kg/d) increases global ａnd tau O-GlcNAc ａnd reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons ａnd hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration ａnd weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain ａnd spinal cord tissues. Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, ａnd knee of the C57BL/6 mice in a dose-dependent manner.

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