2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. PERK

PERK

Protein kinase R-like endoplasmic reticulum kinase; PKR-like endoplasmic reticulum kinase

PERK

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Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is one of four known kinases that respond to cellular stress by deactivating the eukaryotic initiation factor 2 α (eIF2α) or other signal transduction cascades. PERK is highly expressed in pancreatic beta-cells and is essential in the beta-cell's development, differentiation and function.

PERK is a type I ER membrane protein containing a stress-sensing domain facing the ER lumen, a transmembrane segment, and a cytosolic kinase domain. Increase in unfolded proteins in the ER causes release of ER chaperones from the stress-sensing domain of PERK, which results in its activation via oligomerization and autophosphorylation at multiple serine, threonine, and tyrosine residues. Upon activation, PERK phosphorylates eIF2α at serine 51, rendering it an inhibitor of the ribosome translation initiation complex, consequently reducing overall protein synthesis. The reduction in translation reduces the ER burden, providing time for the cell to process or degrade the accumulated unfolded proteins to restore ER homeostasis. Although global protein synthesis is decreased, there is specific increased translation of certain mRNAs, such as ATF4, which modulate cellular survival pathways and enhance UPR function. Interfering with PERK function in cancer cells may limit their ability to thrive under hypoxia or nutrient deprived conditions and lead to apoptosis or tumor growth inhibition.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-124857
    7DG
    		Inhibitor 98%
    7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders.
    7DG
  • HY-175202
    CIDD-8633
    		Inhibitor
    CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 inhibits cell migration and halts the cell cycle and induces apoptosis, significantly suppressing pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 can be used for the study of pancreatic cancer such as PDAC.
    CIDD-8633
  • HY-139612A
    (S)-Opnurasib
    		99.32%
    (S)-Opnurasib ((S)-JDQ-443; (S)-NVP-JDQ443) is an isomer of Opnurasib (HY-139612). Opnurasib is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.
    (S)-Opnurasib
  • HY-153160
    PERK-IN-6
    		Inhibitor 99.46%
    PERK-IN-6 (Compound 5) is a PERK inhibitor with an IC50 of 2.5 nM.
    PERK-IN-6
  • HY-N11011
    Withaphysalin A
    		Inhibitor 98%
    Withaphysalin A is a withanolide compound with anti-inflammatory and antioxidant activities. Withaphysalin A inhibits LPS (HY-D1056)-induced nuclear translocation of NF-κB p65, as well as phosphorylation of STAT3, ERK, JNK and p38 MAPK. Withaphysalin A upregulates the expression of HO-1. Withaphysalin A inhibits LPS-induced production of NO, PGE2, IL-1β, IL-6 and TNF-α. Withaphysalin A downregulates LPS-induced expression of iNOS and COX-2. Withaphysalin A interacts with B-cell activating factor protein (BAFF) to exert inhibitory effects. Withaphysalin A exhibits ELOVL6 inhibitory activity. Withaphysalin A can be used in the research of inflammatory diseases, nephrotic syndrome and chronic myeloid leukemia.
    Withaphysalin A
  • HY-N0265R
    Asperosaponin VI (Standard)
    Asperosaponin VI (Standard) is the analytical standard of Asperosaponin VI. This product is intended for research and analytical applications. Asperosaponin VI is a saponin component from Dipsacus asper. Asperosaponin VI induces osteoblast differentiation through the BMP-2/p38 and ERK1/2 signaling pathways. Asperosaponin VI protects against hypoxia-induced cardiomyocyte apoptosis by activating the PI3K/Akt and CREB pathways. Additionally, Asperosaponin VI also has antidepressant and wound-healing-promoting activities.
    Asperosaponin VI (Standard)
  • HY-W060074
    1-Acetyl-β-carboline
    		Inhibitor
    1-Acetyl-β-carboline is a metabolite of Streptomyces kasugaensis and antibacterial agent. 1-Acetyl-β-carboline increases tyrosinase activity, reduces ERK phosphorylation. 1-Acetyl-β-carboline exhibits antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) strains with MICs ranging from 128 to 256 ug/mL. 1-Acetyl-β-carboline increases the melanin.
    1-Acetyl-β-carboline
  • HY-123037R
    Triadimefon (Standard)
    		Inhibitor
    Triadimefon (Standard) is the analytical standard of Triadimefon (HY-123037). This product is intended for research and analytical applications. Triadimefon is an orally active fungicide. Triadimefon significantly reduces the phosphorylation of AKT1 and ERK1/2. Triadimefon significantly increases pAMPK levels, but does not affect total AMPK levels. Triadimefon inhibits the growth of Saccharomyces cerevisiae, disrupts hormone homeostasis (affecting the synthesis of testosterone, etc.), inhibits fetal adrenal development in rats, induces metabolic shifts in hepatocytes, and impairs spatial learning and memory.
    Triadimefon (Standard)
  • HY-13559
    Atiprimod
    		Activator
    Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML).
    Atiprimod
  • HY-P1120A
    WKYMVm TFA
    		Modulator
    WKYMVm (TFA) is a selective formylpeptide receptor 2 (FPR2) agonist. WKYMVm has a powerful anti-inflammatory effect that can reduce lung injury and spinal cord injury. WKYMVm ameliorates obesity by regulating lipid metabolism and leptin signaling. WKYMVm is involved in the regulation of immune cells by activating FPRs, and WKYMVm can promote the chemotactic migration of immune cells and inhibit the apoptosis of phagocytes. In addition, WKYMVm may play a favorable or unfavorable role in tumors, depending on the type of tumor.
    WKYMVm TFA
  • HY-P990248
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
    		Inhibitor
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is an anti-mouse E-Cadherin/CD324 IgG1 monoclonal antibody. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can downregulate the HER signaling axis and PI3K/Akt/mTOR signaling pathway. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can inhibit the proliferation of tumor cells and induce their apoptosis. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can be used for researches on cancer and inflammation conditions such as breast cancer, chronic compression injury (CCI) and asthma.
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
  • HY-176288
    eIF4E/eIF4G PPI-IN-1
    		Inhibitor
    eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice.
    eIF4E/eIF4G PPI-IN-1
  • HY-173188
    EGFR-IN-154
    		Inhibitor
    EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC50 values of 0.16 μM, 21.73 μM and 41.56 μM against EGFR Del19, EGFR WT and EGFR L858R, respectively. EGFR-IN-154 shows anticancer activity on various cance cell lines. EGFR-IN-154 induces mitochondrial apoptosis, and decreases pERK1/2 and pAkt levels, but increases pJNK and pp38 levels.
    EGFR-IN-154
  • HY-116214S1
    Cyprodinil-13C6
    		Inducer
    Cyprodinil-13C6 (CGA-219417-13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil-<sup>13</sup>C<sub>6</sub>
  • HY-137813S
    PERK-IN-4-d3
    		Inhibitor
    PERK-IN-4-d3 is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
    PERK-IN-4-d<sub>3</sub>
  • HY-145835A
    (S)-PERK-IN-5
    		Inhibitor
    (S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM.
    (S)-PERK-IN-5
  • HY-N0589S
    Dehydrodiisoeugenol-d4
    		Inhibitor
    Dehydrodiisoeugenol-d4 is the deuterium labeled Dehydrodiisoeugenol (HY-N0589). Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.
    Dehydrodiisoeugenol-d<sub>4</sub>
  • HY-144323
    YF135
    		Inhibitor
    YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
    YF135
  • HY-P3395A
    Catestatin sCst
    		Control
    Catestatin sCst is a negative control peptide with a scrambled amino acid sequence. Catestatin sCst fails to activate human mast cells and is used to verify the specificity of Catestatin action.
    Catestatin sCst
  • HY-N3121R
    Pachypodol (Standard)
    		Activator
    Pachypodol (Standard) is the analytical standard of Pachypodol (HY-N3121). This product is intended for research and analytical applications. Pachypodol is an orally active methoxyflavonoid compound. Pachypodol activates the ERK-dependent Nrf2 pathway and inhibits Apoptosis. Pachypodol exhibits activities such as antioxidant, cytoprotective, anti-inflammatory effects. Pachypodol improves cognition. Pachypodol exerts protective effects against cardiac and liver damage. Pachypodol has anticancer activity against colon cancer.
    Pachypodol (Standard)
Cat. No. Product Name / Synonyms Application Reactivity