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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.

Daraxonrasib
RMC-6236, RMC6236, RAS-IN-2
T746982765081-21-6
Daraxonrasib (RMC-6236) is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.
  • $58
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TargetMol | Inhibitor Hot
Zotatifin
eFT226, eFT 226
T172962098191-53-6
Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and anticancer activities, blocking tumor growth driven by receptor tyrosine kinases and inhibiting Sox4 translation, inducing apoptosis.
  • $1,090
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TargetMol | Inhibitor Hot
Rocaglamide
Rocaglamide A, Roc-A
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.
  • $166
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TargetMol | Inhibitor Hot
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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TargetMol | Citations Cited
GCN2iB
T113752183470-12-2
GCN2iB is an ATP-competitive inhibitor of serine/threonine protein kinase, stress-responsive kinase (GCN2), with IC50 of 2.4 nM.
  • $77
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TargetMol | Citations Cited
SHP099
SHP099 free base, SHP-099, SHP 099
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
ATPγS tetralithium salt
ATP-gamma-S tetralithium salt
T2259293839-89-5In house
ATPγS tetralithium salt is a good substrate for RNA-stimulated nucleotide hydrolysis and RNA unwinding activity of eIF4A.
  • $67
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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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Kurarinone
T5S099334981-26-5
Kurarinone is a flavonoid extracted from the shrub Sophora flavescens, which has anti-tumor, estrogenic and anti-inflammatory activities, and also has a strong inhibitory effect on immune responses.
  • $39
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ISRIB (trans-isomer)
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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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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Strictosamide
TN223923141-25-5
Strictosamide possesses antibacterial and antiviral activities, it also may have important effects on inflammation and inflammatory pain.
  • $48
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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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TargetMol | Citations Cited
BTM-3528
BTM3528, BTM 3528
T788752054998-45-5In house
BTM-3528 is an activator of the mitochondrial protease OMA1 with anticancer activity.BTM-3528 activates the ISR via the mitochondrial protease OMA1, inducing OMA1-dependent cleavage of DELE1 and OPA1 and mitochondrial fragmentation.BTM-3528 induces cell growth arrest and apoptosis.
  • $485 TargetMol
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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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HC-5404
HC5404
T865452247396-91-2
HC-5404 is a novel, potent and highly selective PERK (Protein kinase RNA-like Endoplasmic Reticulum Kinase) inhibitor, blocking the activation of the PERK pathway, which in turn inhibits the endoplasmic reticulum stress response signaling pathway, thereby exerting anti-tumor effects, and can be used to treat advanced solid tumors and renal cell Cancer.
  • $179
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DNL343
DNL-343, DNL 343
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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2BAct
2B-Act, 2B Act
T91492143542-28-1
2BAct is a novel eif2b activator, preventing neurological defects caused by a chronic integrated stress response
  • $53
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TargetMol | Citations Cited
Isorhamnetin-3-O-glucoside
Isorhamnetin-3-O-beta-D-Glucoside
T5S19885041-82-7
Isorhamnetin-3-O-glucoside (Isorhamnetin-3-O-beta-D-Glucoside) inhibits the activity of alpha-glucosidase from rat intestine; it exhibits a potent rat lens aldose reductase (RLAR) inhibition in vitro, its IC(50) being 1.4 microM and has inhibitory effects of sorbitol accumulation, suggests that it is a leading compound for further study as a new drug for the prevention and/or treatment of diabetes and its complications.
  • $72
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4EGI-1
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
GCN2-IN-1
A-92
T113731448693-69-3In house
GCN2-IN-1 (A-92) is an effective GCN2 inhibitor and can be utilized in cancer research as a chemotherapeutic agent.
  • $67
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ISRIB
T2027548470-11-7
ISRIB is a potent and selective PERK inhibitor.
  • $48
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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.
  • $30
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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