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-135220
    PERK-IN-2
    		Inhibitor 99.29%
    PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM.
    PERK-IN-2
  • HY-N1500
    Pulegone
    		Inhibitor 99.57%
    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
  • HY-B0168A
    Milnacipran hydrochloride
    		Inhibitor 99.71%
    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 hydrochloride
  • HY-N0687
    Vindoline
    		Inhibitor 99.95%
    Vindoline is an orally active vinca alkaloid. Vindoline can be extracted from the leaves of Catharanthus roseus. Vindoline has a weak inhibitory effect on the self-assembly of tubulin. Vindoline alleviates Apoptosis, inhibits p-p65 and p-ERK. Vindoline improves diabetes, bone loss, osteoarthritis, and kidney damage.
    Vindoline
  • HY-N0777
    Isorhamnetin-3-O-glucoside
    		Activator 99.96%
    Isorhamnetin-3-O-glucoside is an orally active natural compound. Isorhamnetin 3-O-glucoside increases P-ERK, ERK, P-Akt (Ser473), P-PI3K, and PDX-1. Isorhamnetin 3-O-glucoside downregulates C/EBPα and inhibits lipase. Isorhamnetin 3-O-glucoside reduces lipids and inhibits obesity.
    Isorhamnetin-3-O-glucoside
  • HY-101795
    Larixyl acetate
    		Inhibitor 99.46%
    Larixyl acetate is a potent and selective TRPC6 inhibitor with IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.
    Larixyl acetate
  • HY-123205
    Oxatomide
    		Inhibitor 98.11%
    Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.
    Oxatomide
  • HY-N4109
    Decursinol
    		Inhibitor 99.89%
    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
  • HY-137813
    PERK-IN-4
    		Inhibitor 98.21%
    PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
    PERK-IN-4
  • HY-159795
    Claturafenib
    		Inhibitor 99.95%
    Claturafenib ( PF-07799933) is an orally active inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in cells (IC50 value of 1.6 nM in HT29 cells). Claturafenib has anticancer activity against BRAFG469A mutant NSCLC and BRAFK601E mutant melanoma.
    Claturafenib
  • HY-N0924
    (±)-Stylopine
    		Inhibitor 99.86%
    (±)-Stylopine (Tetrahydrocoptisine) is an alkaloid compound. (±)-Stylopine can be isolated from the tubers of the plant Corydalis. (±)-Stylopine inhibits TNF-α, IL-6, and NO production, and attenuates phosphorylation of p38 MAPK, ERK1/2. (±)-Stylopine inhibits NF-κB expression. (±)-Stylopine exhibits anti-inflammatory activity. (±)-Stylopine has protective effects against foot edema, gastric ulcers, anxiety, depression, and acute lung injury.
    (±)-Stylopine
  • HY-N0911
    Rehmannioside A
    		Inhibitor 99.96%
    Rehmannioside A is a compound that can be isolated from Rehmanniae radix. Rehmannioside A is an inhibitor of CYP3A4, 2C9 and 2D6, with IC50 values of 10.08, 12.62 and 16.43 μM, respectively. Rehmannioside A has anti-inflammatory, antioxidant, anti-apoptosis, anti-ferroptosis, cognitive improvement and neuroprotective activities. Rehmannioside A can be used for the research of nervous system and inflammation-related diseases.
    Rehmannioside A
  • HY-101991
    ML291
    		Activator 99.80%
    ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden.
    ML291
  • HY-N6866
    Gomisin N
    		Activator 99.94%
    Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease.
    Gomisin N
  • HY-112056
    DIM-C-pPhCO2Me
    		99.47%
    DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research.
    DIM-C-pPhCO2Me
  • HY-N1198
    Strictosamide
    		Inhibitor 99.91%
    Strictosamide is a compound that can be isolated from Nauclea officinalis. Strictosamide has various activities such as anti-inflammatory, analgesic, anti-Plasmodium, antifungal, and promoting wound healing.
    Strictosamide
  • HY-129138
    Cyanidin 3,5-diglucoside chloride
    		Inhibitor 99.37%
    Cyanidin 3,5-diglucoside chloride is an anthocyanin. Cyanidin 3,5-diglucoside chloride inhibits inflammatory cytokines (IL-1α, IL-1β, and IL-6) expression and NO production. Cyanidin 3,5-diglucoside chloride inhibits the phosphorylation of STAT3, IκB, ERK, p38, and AKT. Cyanidin 3,5-diglucoside chloride inhibits high pressure-induced decrease in GLAST. Cyanidin 3,5-diglucoside chloride exerts anti-inflammatory and skin barrier modulating effects. Cyanidin 3,5-diglucoside chloride can be used in retinal research.
    Cyanidin 3,5-diglucoside chloride
  • HY-N5083
    Saponarin
    		Inhibitor 99.95%
    Saponarin is an orally active flavonoid compound. Saponarin can be isolated from Gypsophila trichotoma. Saponarin inhibits ERK/p38, NF-κB and MAPK phosphorylation and activates AMPK. Saponarin reduces IL-1β and COX-2. Saponarin has antioxidant, anti-inflammatory, hepatoprotective, hypoglycemic and hypotensive effects. Saponarin improves sleep disorders.
    Saponarin
  • HY-50670
    DGAT-1 inhibitor 2
    		Activator
    DGAT-1 inhibitor 2 is an orally active DGAT-1 inhibitor with IC50 values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively. DGAT-1 inhibitor 2 increases ROS concentration, GRP78, and PERK protein abundance. DGAT-1 inhibitor 2 increases SREBF1, CPT1A, and MTTP mRNA in fatty acid-treated cells. DGAT-1 inhibitor 2 improves obesity.
    DGAT-1 inhibitor 2
  • HY-123037
    Triadimefon
    		Inhibitor 98.12%
    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
Cat. No. Product Name / Synonyms Application Reactivity