CHIR-99021 monohydrochloride（又名CHIR99021 monohydrochloride，CT99021 monohydrochloride，CT-99021 monohydrochloride，CT99021 HCl，Laduviglusib monohydrochloride）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 monohydrochloride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 monohydrochloride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 monohydrochloride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 monohydrochloride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.

[2]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.

[3]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29; 7:273.

[4]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10; 5:8566.

冰袋运输。粉末直接保存于-20℃，有效期2年。建议分装后-20℃避光保存，避免反复冻融。