| 名称 | GSK2606414 |
| 描述 | GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase（PERK）inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice. |
| 体外活性 | METHODS: S1-M1-80 vector and S1-M1-80 sgABCG2 cells were treated with GSK2606414 (0.1, 1, 3, 10, 30, 100 μM, 72 hours), and cytotoxicity was determined by MTT assay.
RESULTS GSK2606414 showed dose-dependent cytotoxic effects on both cell lines. [2]
METHODS: N2A cells were treated with GSK2606414 (0.5, 1 μM, 24 hours) and high glucose (30 mM), cells were lysed, and Western blot analysis was performed.
RESULTS N2A cells treated with GSK2606414 reduced the phosphorylation of eIF2α in cells and significantly reduced p-PERK levels in a dose-dependent manner, and GSK2606414 could inhibit the PERK/p-eIF2α/ATF4/CHOP signaling axis. [3] |
| 体内活性 | METHODS: GSK2606414 (50, 150 mg/kg, oral, twice a day, 21 days) was used to treat mice bearing subcutaneous pancreatic human BxPC3 tumors and the effect on tumor growth was observed.
RESULTS GSK2606414 inhibited tumor growth in a dose-dependent manner, with the tumor growth inhibition rates of 20% and 59% at the two doses, respectively. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (110.76 mM), Sonication is recommended.
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| 关键字 | Inhibitor | GSK-2606414 | Apoptosis | Autophagy | PKR-like endoplasmic reticulum kinase | GSK2606414 | GSK 2606414 | inhibit | PERK | Protein kinase R-like endoplasmic reticulum kinase |
| 相关产品 | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
| 相关库 | 高选择性抑制剂库 | 成骨分子库 | 经典已知活性库 | 内质网应激化合物库 | 激酶抑制剂库 | 自噬库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 含氟化合物库 |
United States
