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-N3121
    Pachypodol
    		Activator 99.82%
    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
  • HY-N0412
    Sesamoside
    		Inhibitor 99.77%
    Sesamoside is an orally active anti-inflammatory, anti-hypoxic and analgesic agent. Sesamoside inhibits the phosphorylation of ERK and JNK, downregulates NLRP3 expression, restricts the nuclear localization of P65, regulates AKR1B1 expression, and reduces the expression of TRPV1 gene in the spinal cord. Sesamoside reduces the production of TNF-α, IL-6, IL-1β, iNOS and NO, restores cellular metabolism and organ function, and alleviates cold and mechanical hyperalgesia. Sesamoside can be used in research related to septic shock, high-altitude pulmonary edema and neuropathic pain.
    Sesamoside
  • HY-W923189
    Neral
    		Inhibitor
    Neral is a plant-derived anti-inflammatory, antioxidant and anticancer agent. Neral inhibits the phosphorylation of ERK1/2, p38 MAPK and IκB in macrophages induced by LPS (HY-D1056), suppresses the secretion of TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2 in cells, and reduces the production of ROS in cells. Neral inhibits the activation of the NLRP3 inflammasome, and decreases the activation of caspase-1 and the secretion of IL-1β in mouse macrophages. Neral induces autophagy, and exhibits antiproliferative activity both in in vitro breast cancer cell models and mouse xenograft models. Neral regulates brassinosteroid, jasmonic acid and ethylene signaling pathways, and induces the expression of AP2/ERF-ERF and bHLH family genes in rice roots. Neral acts as a herbicide safener, alleviates the damage induced by Fenoxaprop-P-ethyl (HY-B2013), and promotes the elongation of rice roots. Neral can be used in research related to breast cancer, inflammatory and immune system diseases, and herbicide safeners.
    Neral
  • HY-156625
    Nedometinib
    		Inhibitor 98.09%
    Nedometinib (NFX-179) is a specific MEK1 inhibitor with an IC50 of 135 nM. Nedometinib inhibits p-ERK, MAPK. Nedometinib exerts anticancer activity against squamous cell carcinoma. Nedometinib can be used for research in dermatosis, neurofibromatosis.
    Nedometinib
  • HY-P1421
    Obestatin(human)
    		Activator 99.74%
    Obestatin(human) is a 23-amino acid amidated peptide that regulates appetite and gastrointestinal motility via its interaction with GPR39. Obestatin(human) can be used for weight loss. Obestatin(human) cannot penetrate the cell membrane.
    Obestatin(human)
  • HY-164315
    KRAS G12C inhibitor 67
    		Inhibitor 98.80%
    KRAS G12C inhibitor 67 (Example 35) is an orally active KRAS G12C inhibitor. KRAS G12C inhibitor 67 inhibits pERK and active KRas. KRAS G12C inhibitor 67 selectively inhibits the growth of various KRAS G12C mutant tumor cell lines. KRAS G12C inhibitor 67 exhibits anticancer activity against esophageal cancer, bladder cancer, colorectal cancer, lung cancer, and pancreatic cancer.
    KRAS G12C inhibitor 67
  • HY-P991571
    GC1118
    		Inhibitor
    GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer.
    GC1118
  • HY-N6908
    Continentalic acid
    		Modulator 99.72%
    Continentalic acid is a diterpenoid organic acid. Continentalic acid exhibits multiple activities including anti-inflammatory, antioxidant, neuroprotective, antibacterial and antitumor effects. Continentalic acid alleviates oxidative stress, reduces pro-inflammatory cytokine production, inhibits MAPK phosphorylation and neutrophil infiltration, and induces growth inhibition and apoptosis of cancer cells. Continentalic acid can be used in research related to traumatic brain injury, cancer, inflammation and infections.
    Continentalic acid
  • HY-B1428
    2-Ethoxybenzamide
    		99.82%
    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
  • HY-162445
    KRASG12D-IN-3
    		Inhibitor 98.38%
    KRASG12D-IN-3 is an orally active KRASG12D inhibitor. KRASG12D-IN-3 inhibits the growth of gastric cancer and pancreatic cancer cells. KRASG12D-IN-3 inhibits the activity of p-ERK in gastric cancer cells. KRASG12D-IN-3 can be used for the research of gastric cancer and pancreatic cancer.
    KRASG12D-IN-3
  • HY-176498
    NBM-T-BMX-OS01
    		Inhibitor 99.74%
    NBM-T-BMX-OS01 is an Osthole (HY-N0054) derivative. NBM-T-BMX-OS01 inhibits the phosphorylation of VEGFR2, FAK, Akt and ERK. NBM-T-BMX-OS01 has anti-angiogenic activity. NBM-T-BMX-OS01 has anti-cancer activity against colorectal cancer.
    NBM-T-BMX-OS01
  • HY-114978
    VU0424465
    		Agonist 99.84%
    VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.
    VU0424465
  • HY-155068
    FC-116
    		Inhibitor 98.04%
    FC-11 is a tubulin inhibitor. FC-116 inhibits the proliferation of colorectal cancer (CRC) cells, with IC50 values of 4.52 nM for HCT116 cells and 18.69 nM for CT26 cells. FC-11 can induce ER stress to generate excess ROS, leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-116 exerts potent anti-tumor effects in vivo. FC-11 can be used for the study of colorectal cancer.
    FC-116
  • HY-B0168
    Milnacipran
    		Inhibitor 99.69%
    Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia).
    Milnacipran
  • HY-145835
    PERK-IN-5
    		Inhibitor 99.07%
    PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
    PERK-IN-5
  • HY-148821
    BJG-05-039
    		Inhibitor
    BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 (HY-100519) conjugated to Lenalidomide (HY-A0003). BJG-05-039 induces selective degradation of PAK1. BJG-05-039 inhibits phosphorylation of MEK S298, as well as inhibiting phosphorylation of ERK. BJG-05-039 has an anti-proliferative effect on PAK1-dependent cell lines.
    BJG-05-039
  • HY-175504
    MLS6357
    		Antagonist 99.57%
    MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.
    MLS6357
  • HY-134811
    KRAS G12D inhibitor 1
    		Inhibitor
    KRAS G12D inhibitor 1 is a KRASG12D inhibitor with an IC50 value of 0.4 nM. KRAS G12D inhibitor 1 inhibits KRasG12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 can be used for cancer research.
    KRAS G12D inhibitor 1
  • HY-13699
    NBI-42902
    		Inhibitor 98.65%
    NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
    NBI-42902
  • HY-116214R
    Cyprodinil (Standard)
    		Inducer
    Cyprodinil (Standard) (CGA-219417 (Standard)) is the analytical standard of Cyprodinil (HY-116214). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity