PERK
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S7307 | GSK2606414 | <1 mg/mL | 90 mg/mL | 19 mg/mL |
| S7033 | GSK2656157 | <1 mg/mL | 32 mg/mL | <1 mg/mL |
| S7400 | ISRIB (trans-isomer) | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S2923 | Salubrinal | <1 mg/mL | 95 mg/mL | 2 mg/mL |
| S7437 | Sal003 | <1 mg/mL | 93 mg/mL | <1 mg/mL |
| S8304 | Azoramide | <1 mg/mL | 61 mg/mL | 61 mg/mL |
- PERK抑制剂（6）
| 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。 |
C. PERK inhibitor (PERKi, GSK2606414) partially reverted vemurafenib-induced autophagy. BCPAP cells were treated with 5 M PLX and/or 1 M PERKi for 24 hours. After that, protein lysates were prepared and subjected to immunoblotting against the indicated antibodies. Relative quantity of LC3II/LC3I was calculated by ImageJ densitometric analysis and normalized to control (DMSO/DMSO PERKi).
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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。 |
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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。 |
