PERK

ATPγS tetralithium salt is a substrate for nucleotide hydrolysis and RNA unraveling activity of the eukaryotic translation initiation factor eIF4A, associated with p97 mutants and prions.

CCT020312 is a selective activator of EIF2AK3 and PERK. CCT020312 durably inhibits cell proliferation and elicits the phosphorylation of EIF2A.

4EGI-1, a competitive eIF4E/eIF4 g interaction inhibitor, binds to eIF4E(KD=25 μM).

AMC-01 has potential antiviral activity and induces dose- and time-dependent inactivation of eIF2-α via phosphorylation of serine residue 51. AMC-01 can be used to study atherosclerosis and Parkinson's syndrome.

PERK-IN-4 is a potent and selective PERK inhibitor with an IC50 value of 0.3 nM.PERK-IN-4 can be used in the study of cancer and neurological disorders.

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist.MSU-42011 potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level.MSU-42011 has demonstrated antitumor activity in a kras-driven mouse model of lung cancer.MSU-42011 is an effective therapy for the treatment of preclinical krasdriven lung cancer and has immunomodulatory activity.

PERK-IN-6 is a novel and highly potent PERK inhibitor (IC50:2.5 nM).

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

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) that induces autophagy.AMG PERK 44 inhibits GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM) and can be used in the study of cancer.

ISRIB is a potent and selective PERK inhibitor.

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

GSK2606414 is an oral-available and specific PERK inhibitor (IC50=0.4 nM).

2BAct is a novel eif2b activator, preventing neurological defects caused by a chronic integrated stress response

4E2RCat is an eIF4E-eIF4G interaction inhibitor (IC50: 13.5 μM).

4E1RCat is a dual inhibitor of eIF4E:eIF4 g and eIF4E:4E-BP1 interaction. And it inhibits the binding of eIF4 g to eIF4E with IC50 of 3.2 μM.

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

Briciclib (ON 014185) is a small molecule that suppresses cyclin D1 accumulation in Y cells.

MK-28 is a selective PERK agonist that reduces toxicity and prolongs survival in a Huntington's disease model.MK-28 has a significant killing effect on MK28 gastric cancer cells.

SBI-0640756 (SBI-756) (SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.

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

SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.

BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor that induces pERK activation.BAY 2965501 can be used in the study of cancer.

Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.

Azoramide, a small-molecule modulator, has the antidiabetic activity of unfolded protein response.

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