PERK

抑制剂选择性比较

PERK产品

所有产品 PERK抑制剂(3) PERK调节剂(3)

产品目录	产品描述	文献引用	实验数据
S7307	GSK2606414 GSK2606414 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。	Mol Cell Endocrinol, 2020, 499:110595 Autophagy, 2019, 10.1080/15548627.2019.1606647 Metabolism, 2019, 97:87-91	GSK2606414 decreased the number of TUNEL-positive neurons at 72 h after SAH. Representative microphotographs showed the colocalization of NeuN (red) with TUNEL (green)-positive cells in the bilateral basal cerebral cortex at 72 h after SAH (a). Quantitative analysis of TUNEL-positive neurons showed that GSK2606414 decreased the number of apoptotic cells after SAH (b). Scale bar=100 μm, *p < 0.05 versus sham; #p < 0.05 versus SAH + vehicle; ξp < 0.05 versus SAH+GSK2606414 (30 μg).
S7033	GSK2656157 GSK2656157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。	Metabolism, 2019, 97:87-91 Cell Death Dis, 2019, 10(9):651 Biomed Pharmacother, 2019, 109:254-261	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。	Development, 2017, 144(1):128-138 eNeuro, 2017, 4(4)	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.
S2923	Salubrinal Salubrinal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。	Mol Hum Reprod, 2019, 10.1093/molehr/gaz002 DNA Cell Biol, 2019, 10.1089/dna.2019.5097 Mol Nutr Food Res, 2018, 62(8):e1700890	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	Sal003 Sal003 是一种有效的细胞渗透性eIF-2α phosphatase抑制剂。
S8304	Azoramide Azoramide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	GSK2606414 GSK2606414 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。	Mol Cell Endocrinol,2020, 499:110595 Autophagy,2019, 10.1080/15548627.2019.1606647 Metabolism,2019, 97:87-91	GSK2606414 decreased the number of TUNEL-positive neurons at 72 h after SAH. Representative microphotographs showed the colocalization of NeuN (red) with TUNEL (green)-positive cells in the bilateral basal cerebral cortex at 72 h after SAH (a). Quantitative analysis of TUNEL-positive neurons showed that GSK2606414 decreased the number of apoptotic cells after SAH (b). Scale bar=100 μm, *p < 0.05 versus sham; #p < 0.05 versus SAH + vehicle; ξp < 0.05 versus SAH+GSK2606414 (30 μg).
S7033	GSK2656157 GSK2656157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。	Metabolism,2019, 97:87-91 Cell Death Dis,2019, 10(9):651 Biomed Pharmacother,2019, 109:254-261	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。	Development,2017, 144(1):128-138 eNeuro,2017, 4(4)	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

S7307

GSK2606414

GSK2606414 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。

Mol Cell Endocrinol,2020, 499:110595

Autophagy,2019, 10.1080/15548627.2019.1606647

Metabolism,2019, 97:87-91

S7033

GSK2656157

GSK2656157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。

Metabolism,2019, 97:87-91

Cell Death Dis,2019, 10(9):651

Biomed Pharmacother,2019, 109:254-261

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。

Development,2017, 144(1):128-138

eNeuro,2017, 4(4)

产品目录	产品描述	文献引用	实验数据
S2923	Salubrinal Salubrinal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。	Mol Hum Reprod, 2019, 10.1093/molehr/gaz002 DNA Cell Biol, 2019, 10.1089/dna.2019.5097 Mol Nutr Food Res, 2018, 62(8):e1700890	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	Sal003 Sal003 是一种有效的细胞渗透性eIF-2α phosphatase抑制剂。
S8304	Azoramide Azoramide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

S2923