|S2923||Salubrinal||<1 mg/mL||95 mg/mL||2 mg/mL|
|S7307||GSK2606414||<1 mg/mL||90 mg/mL||19 mg/mL|
|S7033||GSK2656157||<1 mg/mL||32 mg/mL||<1 mg/mL|
|S7437||Sal003||<1 mg/mL||93 mg/mL||<1 mg/mL|
|S7400||ISRIB (trans-isomer)||<1 mg/mL||4 mg/mL||<1 mg/mL|
|S8304||Azoramide||<1 mg/mL||61 mg/mL||61 mg/mL|
Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
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)
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.
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).
GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases.
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.
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells.
Azoramide is a small-molecule modulator of the unfolded protein response (UPR). It improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress.