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PERK

protein kinase R-like endoplasmic reticulum kinase (PERK), inositol-requiring kinase 1 (IRE1) and activating transcription factor 6 (ATF6). Consequently, the harmful stimuli from the ER stress transducers induce apoptosis and autophagy, which share several crosstalks and eventually decide the cell fate.

  • ATPγS tetralithium salt
    T2259293839-89-5In house
    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.
    • $148
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    TargetMol | Inhibitor Hot
  • CCT020312
    T14902324759-76-4In house
    CCT020312 is a selective activator of EIF2AK3 and PERK. CCT020312 durably inhibits cell proliferation and elicits the phosphorylation of EIF2A.
    • $63
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    TargetMol | Inhibitor Hot
  • 4EGI-1
    T2665315706-13-9
    4EGI-1, a competitive eIF4E/eIF4 g interaction inhibitor, binds to eIF4E(KD=25 μM).
    • $37
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    TargetMol | Citations Cited
  • AMC-01
    T299551047978-71-1In house
    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.
    • $350
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  • PERK-IN-4
    T387321337531-89-1In house
    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.
    • $59
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  • MSU-42011
    T774992456434-36-7In house
    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.
    • $41
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  • PERK-IN-6
    T720531337532-14-5In house
    PERK-IN-6 is a novel and highly potent PERK inhibitor (IC50:2.5 nM).
    • $162
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  • GCN2-IN-6
    T113742183470-09-7In house
    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
    • $117
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    TargetMol | Inhibitor Sale
  • GP 1a
    T41231511532-96-0In house
    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.
    • $51
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  • AMG PERK 44
    T102991883548-84-2In house
    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.
    • $52
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  • 4E1rcat
    T1742328998-25-0
    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.
    • $47
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    TargetMol | Citations Cited
  • GSK2656157
    T26541337532-29-2
    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.
    • $32
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    TargetMol | Citations Cited
  • ISRIB
    T2027548470-11-7
    ISRIB is a potent and selective PERK inhibitor.
    • $48
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    TargetMol | Citations Cited
  • SHP099
    T35641801747-42-1
    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.
    • $31
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    TargetMol | Citations Cited
  • Salubrinal
    T3045405060-95-9
    Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α).
    • $35
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    TargetMol | Citations Cited
  • GSK2606414
    T26141337531-36-8
    GSK2606414 is an oral-available and specific PERK inhibitor (IC50=0.4 nM).
    • $61
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    TargetMol | Citations Cited
  • 4E2RCat
    T14044432499-63-3
    4E2RCat is an eIF4E-eIF4G interaction inhibitor (IC50: 13.5 μM).
    • $97
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  • Briciclib
    T3207865783-99-9
    Briciclib (ON 014185) is a small molecule that suppresses cyclin D1 accumulation in Y cells.
    • $39
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  • BTdCPU
    T71501257423-87-2
    BTdCPU is a potent activator of heme-regulated eIF2α kinase (HRI) . BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
    • $148
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  • 2BAct
    T91492143542-28-1
    2BAct is a novel eif2b activator, preventing neurological defects caused by a chronic integrated stress response
    • $53
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  • MK-28
    T61859864388-65-8
    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.
    • $100
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  • Vaccarin
    T388153452-16-7
    Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.
    • $130
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  • SBI-0640756
    T51731821280-29-8
    SBI-0640756 (SBI-756) (SBI-756) is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
    • $55
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  • ISRIB (trans-isomer)
    T61831597403-47-8
    ISRIB (trans-isomer) (ISRIB trans-isomer), the trans-isomer of ISRIB, is a effective and specific PERK inhibitor (IC50: 5 nM).
    • $31
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  • BAY 2965501
    T730532732902-08-6
    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.
    • $84
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  • Rocaglamide
    TQ013184573-16-0
    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.
    • $849
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  • Sal003
    T24171164470-53-4
    Sal003, an effective cell-permeable analog, inhibitis the eIF2α phosphatase.
    • $32
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  • Azoramide
    T4304932986-18-0
    Azoramide, a small-molecule modulator, has the antidiabetic activity of unfolded protein response.
    • $43
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