eif2α

EIF2α Activator 1 (Compound 40) is a chemical compound that activates the phosphorylation of eukaryotic initiation factor 2 alpha (eIF2α), enhancing the expression of downstream proteins ATF and CHOP. It demonstrates antiproliferative effects against K562 and PBMC cells, with IC50 values of 4.00 and 19.3 μM, respectively [1].

EIF2α activator 2 (Compound 1) is a phosphorylated activator of eukaryotic initiation factor 2α (eIF2α). EIF2α activator 2 is anti-proliferative in K562 cells (IC50: 4.79 μM) and PBMC cells (IC50: 10.52 μM).

GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells). GCN2-IN-6  is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9

Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α).

BTdCPU is a potent activator of heme-regulated eIF2α kinase (HRI) . BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.

Icerguastat (IFB-088) is a selective inhibitor of holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo.

Sal003, an effective cell-permeable analog, inhibitis the eIF2α phosphatase.

GSK621 is a specific and potent AMPK activator.

Avarol induces apoptosis in pancreatic ductal adenocarcinoma cells by activating PERK-eIF2α-CHOP signaling. Avarl also acts as a competitive AChE inhibitor which are non-hepatotoxic and neuroprotective agents for Alzheimer's disease.

N1-Methylpseudouridine (1-Methylpseudouridine) is a methylpseudouridine and enhances translation through eIF2α-dependent and independent mechanisms by increasing ribosome density in mRNA.

PERK-IN-5 is a highly selective, potent, orally active inhibitor of the protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) that acts on PERK (IC50: 2 nM) and p-eIF2α (IC50: 9 nM). PERK-IN-5 significantly inhibited tumour growth in the 786-O renal cell carcinoma xenograft tumour model.

ISRIB (trans-isomer) (ISRIB trans-isomer), the trans-isomer of ISRIB, is a effective and specific PERK inhibitor (IC50: 5 nM).

Sephin1 hydrochloride is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A), which prolongs the benefit of eIF2α phosphorylation, thereby protecting cells from proteostatic defects.

Sephin1 (IFB-088) is reportedly a selective inhibitor of GADD34 (PPP1R15A), which is a stress-induced regulatory subunit of protein phosphatase 1 complex that dephosphorylates eIF2α