PERK
抑制剂选择性比较
PERK产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7307 |
GSK2606414GSK2606414 是一种口服具有生物活性的，有效的，选择性PERK抑制剂，IC50 为 0.4 nM，比测试的其他EIF2AKs选择性至少高100倍。 |
Representative westerns and summary results showing decreased eIf2α phospho-immunoreactivity (Phos) following intracerebroventricular administration of GSK2606414 (or vehicle) to uninjured mice (n = 4/group). The total levels of eIF2α did not change as a result of treatment. When calculated as a phospho–total ratio (P/T), a significant decrease in phosphorylation was observed in mice treated with GSK2606414. *p < 0.05 between vehicle and drug-treated animals.
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| S7033 |
GSK2656157GSK2656157是一种ATP竞争性的高选择性PERK抑制剂，无细胞试验中IC50为0.9 nM, 比作用于一组300种激酶选择性高500多倍。 |
GSK2656157 inhibits excessive autophagy in kri1lcas002 HSPCs. Representative confocal images of mCherry-Lc3 puncta (autophagosomes) in kri1lcas002 mutant embryos in Tg (cmyb: egfp) transgenic background are shown. Scale bars, 5 μm.
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| S7400 |
ISRIB (trans-isomer)ISRIB(trans-isomer), 反式异构体ISRIB, 是一种高度选择性PERK抑制剂，其IC50为5 nM. 对非应激细胞的翻译、转录或是mRNA的稳定性没有广泛作用。 |
PERK inhibitor treatment restores female development in zar1 homozygous mutants. Juveniles were treated with two PERK inhibitors from 22 dpf to 60 dpf. Final concentration: ISRIB, 50 nM. **P<0.01, ***P<0.001.
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| S2923 |
SalubrinalSalubrinal是一种选择性eIF2α去磷酸化抑制剂，可以抑制ER应激介导的细胞凋亡，无细胞试验中EC50约为15 μM。 |
AngII (30 minutes)-induced Akt activation was attenuated by the ER stress inhibitors 4-PBA (5 mM, 2 hours), TUDCA (300 µg/ml, 1 hour), and salubrinal (30 µM, 1 hour) (n=5; *P<0.01 versus con, #P<0.05 versus Ang) |
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| S7437 |
Sal003Sal003 是一种有效的细胞渗透性eIF-2α phosphatase抑制剂。 |
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| S8304 |
AzoramideAzoramide是非折叠蛋白质应答UPR的小分子调节剂，可改善内质网蛋白折叠能力，激活ER伴侣蛋白能力，保护蛋白免受内质网应激反应。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7307 |
GSK2606414GSK2606414 是一种口服具有生物活性的，有效的，选择性PERK抑制剂，IC50 为 0.4 nM，比测试的其他EIF2AKs选择性至少高100倍。 |
Representative westerns and summary results showing decreased eIf2α phospho-immunoreactivity (Phos) following intracerebroventricular administration of GSK2606414 (or vehicle) to uninjured mice (n = 4/group). The total levels of eIF2α did not change as a result of treatment. When calculated as a phospho–total ratio (P/T), a significant decrease in phosphorylation was observed in mice treated with GSK2606414. *p < 0.05 between vehicle and drug-treated animals.
|
|
| S7033 |
GSK2656157GSK2656157是一种ATP竞争性的高选择性PERK抑制剂，无细胞试验中IC50为0.9 nM, 比作用于一组300种激酶选择性高500多倍。 |
GSK2656157 inhibits excessive autophagy in kri1lcas002 HSPCs. Representative confocal images of mCherry-Lc3 puncta (autophagosomes) in kri1lcas002 mutant embryos in Tg (cmyb: egfp) transgenic background are shown. Scale bars, 5 μm.
|
|
| S7400 |
ISRIB (trans-isomer)ISRIB(trans-isomer), 反式异构体ISRIB, 是一种高度选择性PERK抑制剂，其IC50为5 nM. 对非应激细胞的翻译、转录或是mRNA的稳定性没有广泛作用。 |
PERK inhibitor treatment restores female development in zar1 homozygous mutants. Juveniles were treated with two PERK inhibitors from 22 dpf to 60 dpf. Final concentration: ISRIB, 50 nM. **P<0.01, ***P<0.001.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2923 |
SalubrinalSalubrinal是一种选择性eIF2α去磷酸化抑制剂，可以抑制ER应激介导的细胞凋亡，无细胞试验中EC50约为15 μM。 |
AngII (30 minutes)-induced Akt activation was attenuated by the ER stress inhibitors 4-PBA (5 mM, 2 hours), TUDCA (300 µg/ml, 1 hour), and salubrinal (30 µM, 1 hour) (n=5; *P<0.01 versus con, #P<0.05 versus Ang) |
|
| S7437 |
Sal003Sal003 是一种有效的细胞渗透性eIF-2α phosphatase抑制剂。 |
||
| S8304 |
AzoramideAzoramide是非折叠蛋白质应答UPR的小分子调节剂，可改善内质网蛋白折叠能力，激活ER伴侣蛋白能力，保护蛋白免受内质网应激反应。 |
