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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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  • GSK2606414
    T26141337531-36-8
    GSK2606414 is an oral-available and specific PERK inhibitor (IC50=0.4 nM).
    • $61
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  • 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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  • DNL343
    T788762278265-85-1In house
    DNL343 is a selective and potent eIF2B activator that crosses the blood-brain barrier and inhibits the assembly of stress granules (SGs) induced by the C9ORF72 dipeptide repeats. DNL343 may be useful in the study of neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS).
    • $148 TargetMol
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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, and it can be utilized in cancer research.
    • $84
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  • 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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  • ISRIB
    T2027548470-11-7
    ISRIB is a potent and selective PERK inhibitor.
    • $48
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  • ISRIB (trans-isomer)
    T61831597403-47-8
    ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α.
    • $31
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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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  • 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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  • 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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  • 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.
    • $299
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  • 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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  • Sal003
    T24171164470-53-4
    Sal003, an effective cell-permeable analog, inhibitis the eIF2α phosphatase.
    • $32
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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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  • 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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  • 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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  • 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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  • Vaccarin
    T388153452-16-7
    Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.
    • $44
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  • Briciclib
    T3207865783-99-9
    Briciclib (ON 014185) is a small molecule that inhibits cyclin D1 accumulation in Y cells.
    • $29
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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. It also inhibits GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM), making it useful for cancer research.
    • $52
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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, used in the study of cancer and neurological disorders.
    • $59
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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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  • MSU-42011
    T774992456434-36-7In house
    MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It 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 and is effective for the treatment of preclinical [kras]-driven lung cancer with 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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  • 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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  • 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.
    • $33
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  • 4E2RCat
    T14044432499-63-3
    4E2RCat is an inhibitor of eIF4E-eIF4G interaction (IC50 = 13.5 μM) and effectively blocks coronavirus replication, as evidenced by reduced viral protein expression and decreased production of infectious virus.
    • $58
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  • Azoramide
    T4304932986-18-0
    Azoramide, a small-molecule modulator, has the antidiabetic activity of unfolded protein response.
    • $31
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  • eIF4A3-IN-1
    T111702095486-67-0
    eIF4A3-IN-1 is a selective and potent inhibitor of eukaryotic initiation factor 4A3 (eIF4A3) with an IC50 value of 0.26 μM. eIF4A3-IN-1 inhibits cytosolic nonsense-mediated RNA decay at high concentrations.
    • $142
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