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-18318
    Takeda-6D
    		Inhibitor
    Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.
    Takeda-6D
  • HY-144692
    MEK/PI3K-IN-1
    		Inhibitor
    MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.
    MEK/PI3K-IN-1
  • HY-N0231R
    Bavachalcone (Standard)
    		Inhibitor
    Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro.
    Bavachalcone (Standard)
  • HY-152168
    NSC 295642
    NSC 295642 is a phosphatase inhibitor. NSC 295642 can significantly increase phospho-Erk cytonuclear differences in intact cells. NSC 295642 can be used for the research of cancer.
    NSC 295642
  • HY-N4109R
    Decursinol (Standard)
    		Inhibitor
    Decursinol (Standard) is the analytical standard of Decursinol (HY-N4109). This product is intended for research and analytical applications. Decursinol is an orally active coumarin compound that can be isolated from the roots of Angelica gigas. Decursinol is also a metabolite of Decursin (HY-18981) and Decursinol angelate (HY-N4322). Decursinol exhibits multiple activities such as analgesic, antinociceptive, anti-inflammatory, antioxidant, antimetastatic, and neuroprotective effects. Decursinol can be used for research on diseases such as tumors and nervous system disorders.
    Decursinol (Standard)
  • HY-124857
    7DG
    		Inhibitor 98%
    7DG (7-Desacetoxy-6,7-dehydrogedunin) is a protein kinase R (PKR) inhibitor. 7DG protects macrophages from lethal toxin-induced pyroptosis.
    7DG
  • HY-116214S
    Cyprodinil-d5
    		Inducer
    Cyprodinil-d5(CGA-219417-d5) is the deuterium 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-d<sub>5</sub>
  • HY-173153
    BRAFV600E/JNK-IN-1
    		Inhibitor
    BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities.
    BRAFV600E/JNK-IN-1
  • HY-P10780
    RFRP-3 (mouse)
    		Inhibitor
    RFRP-3 (mouse) is a functional ortholog of avian gonadotropin inhibitory hormone (GnIH), binding to GPR147. RFRP-3 (mouse) reduces Progesterone synthesis by inhibiting FSHR and key enzymes involved in steroidogenesis (P450scc, 3β-HSD, StAR). RFRP-3 (mouse) induces Apoptosis (increase of p53). RFRP-3 (mouse) also suppresses the ERK signaling pathway. RFRP-3 (mouse) can be used for research of follicular development.
    RFRP-3 (mouse)
  • HY-168442
    KRAS inhibitor-40
    		Inhibitor
    KRAS inhibitor-40 (Compound 41) is a KRAS inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of KRAS downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different KRAS mutation types and has antitumor activity.
    KRAS inhibitor-40
  • HY-168493
    FLT3/VEGFR2-IN-1
    		Inhibitor
    FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia.
    FLT3/VEGFR2-IN-1
  • HY-130643
    PERK-IN-3
    		Inhibitor
    PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM.
    PERK-IN-3
  • HY-153160
    PERK-IN-6
    		Inhibitor 99.82%
    PERK-IN-6 (Compound 5) is a PERK inhibitor with an IC50 of 2.5 nM.
    PERK-IN-6
  • HY-110198
    ONO-8130
    		Inhibitor
    ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research.
    ONO-8130
  • HY-B0168AS
    Milnacipran-d5 hydrochloride
    		Inhibitor
    Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia).
    Milnacipran-d<sub>5</sub> hydrochloride
  • HY-N1500S1
    Pulegone-d8
    		Inhibitor
    Pulegone-d8 is deuterated labeled Pulegone (HY-N1500). Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.
    Pulegone-d<sub>8</sub>
  • 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-B0168S
    Milnacipran-d10 hydrochloride
    		Inhibitor
    Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia).
    Milnacipran-d<sub>10</sub> hydrochloride
  • HY-N1500R
    Pulegone (Standard)
    		Inhibitor
    Pulegone (Standard) is the analytical standard of Pulegone (HY-N1500). This product is intended for research and analytical applications. Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.
    Pulegone (Standard)
  • HY-B1428R
    2-Ethoxybenzamide (Standard)
    2-Ethoxybenzamide (Standard) is the analytical standard of 2-Ethoxybenzamide (HY-B1428). 2-Ethoxybenzamide (Ethenzamide) is a nonsteroidal anti-inflammatory agent that shows analgesic and antipyretic effects. 2-Ethoxybenzamide induces melanin synthesis via cAMP response element-binding protein (CREB) phosphorylation. 2-Ethoxybenzamide can be used in the research of hypopigmentation and inflammation-related diseases.
    2-Ethoxybenzamide (Standard)
Cat. No. Product Name / Synonyms Application Reactivity