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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 good substrate for RNA-stimulated nucleotide hydrolysis and RNA unwinding activity of eIF4A.
  • $148
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GSK2606414
T26141337531-36-8
GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase(PERK)inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice.
  • $61
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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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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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CCT020312
T14902324759-76-4In house
CCT020312 (0-9 µM, 24 h) treatment of medium HT29 cells for 24 h resulted in a concentration-dependent loss of P-S608-pRB signaling with linear response values between 1.8 and 6.1 µM.
  • $56
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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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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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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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ISRIB
T2027548470-11-7
ISRIB is a potent and selective PERK inhibitor.
  • $48
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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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Sal003
T24171164470-53-4
Sal003, an effective cell-permeable analog, inhibitis the eIF2α phosphatase.
  • $32
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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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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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Briciclib
T3207865783-99-9
Briciclib (ON 014185) is a small molecule that inhibits cyclin D1 accumulation in Y cells.
  • $39
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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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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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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.
  • $89
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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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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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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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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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GCN2-IN-7
T636992396465-33-9In house
GCN2-IN-7 is an orally active, potent and selective inhibitor of the environmental sensing protein GCN2 with anti-tumor activity and can be used to study melanoma.
  • $313
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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.
  • $355
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HC-5404-Fu
T2001113034479-99-4
HC-5404-Fu is an inhibitor of PERK with anti-tumor activity. This compound inhibits the signaling pathway of the endoplasmic reticulum stress response. Additionally, HC-5404-Fu increases the sensitivity of renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). It holds potential for research into renal cell carcinoma, stomach cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.
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10-14 weeks
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