GCN2-IN-6 (Compound 6d) 是一种有效的口服 GCN2 抑制剂，通过酶法 (IC50 为 1.8 nM) 和细胞分析 (IC50 为 9.3 nM) 证实。GCN2-IN-6 还是 eIF2α 激酶 PERK 抑制剂，IC50 为 0.26 nM (酶法测定) 和 230 nM (细胞测定)。
货号:ajcx16528
CAS:2183470-09-7
分子式:C19H12Cl2F2N4O3S
分子量：485.29
溶解度:DMSO: 250 mg/mL (515.16 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells)[1].

[1]. Fujimoto J, et al. Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode. ACS Med Chem Lett. 2019 Sep 19;10(10):1498-1503.