CHIR-99021 trihydrochloride（又名CHIR99021 trihydrochloride，CT99021 trihydrochloride，CT-99021 trihydrochloride，Laduviglusib trihydrochloride）是一种有效的、选择性、特异性较高的糖原合酶激酶-3（GSK-3α/β）抑制剂（IC₅₀值分别为10 nM和6.7 nM），其对CDC2、ERK2和GSK-3等蛋白激酶也有抑制作用。此外，CHIR-99021也是一种有效的Wnt/β-catenin信号通路激活剂，其在非小细胞肺癌（NSCLC）细胞中上调cyclin A表达并促进细胞增殖。CHIR-99021通过调节转化生长因子β（TGF-β）和丝裂原活化蛋白激酶（MAPK）等信号通路而促进小鼠或人胚胎干细胞的自我更新。CHIR-99021稳定下游效应子c-Myc和β-catenin，从而促进B6和BALB/c ES细胞的自我更新，维持细胞多能性。CHIR-99021能诱导细胞自噬(autophagy)。

参考文献

[1]. Ma Y, Ma M, Sun J, Li W, Li Y, Guo X, Zhang H. CHIR-99021 regulates mitochondrial remodelling via β-catenin signalling and miRNA expression during endodermal differentiation. J Cell Sci. 2019 Jul 31;132(15): jcs229948.

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