PERK
Protein kinase R-like endoplasmic reticulum kinase; PKR-like endoplasmic reticulum kinase
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.
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PERK Related Products (221)
Related Products (221)
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Antibodies (2)
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EGFR-IN-175
0 ImagesCat. No.: HY-178009EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor with an IC50 of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer.
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Vernodalin
0 ImagesCat. No.: HY-N19029CAS No.: 21871-10-3Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a Kd value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.
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MEK/PI3K-IN-1
0 ImagesCat. No.: HY-144692CAS No.: 2281803-28-7
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Daraxonrasib-d5
0 ImagesCat. No.: HY-148439SSynonyms: RMC-6236-d5; RAS-IN-2-d5Daraxonrasib-d5 (RMC-6236-d5) is the deuterated-labeled Daraxonrasib (HY-148439). Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors.
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GAT100
0 ImagesCat. No.: HY-120093CAS No.: 1663564-42-8GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases.
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Bavachalcone (Standard)
0 ImagesCat. No.: HY-N0231RCAS No.: 28448-85-3Synonyms: Broussochalcone B (Standard)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.
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NSC 295642
0 ImagesCat. No.: HY-152168CAS No.: 77111-29-6NSC 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.
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MEK-IN-10
0 ImagesCat. No.: HY-183674CAS No.: 3096958-11-8MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer.
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Gy-CATH
0 ImagesCat. No.: HY-P11467Gy-CATH is an anionic antimicrobial peptide. Gy-CATH activates MAPK and NF-κB signaling pathways (elevated levels of phospho-ERK, -p38, -JNK, -p65, and -IκBα). Gy-CATH upregulates the expression levels of three physiological anticoagulant pathways. Gy-CATH inhibits ADP-, Collagen-, and PMA-induced platelet aggregation. Gy-CATH has no direct antimicrobial activity, but shows significant preventive abilities against mice infected with Staphylococcus aureus, Escherichia coli, and Methicillin (HY-121544)-resistant Staphylococcus aureus. Gy-CATH exhibits potent immunomodulatory activity, enhancing macrophage-and neutrophil-mediated bactericidal functions. Gy-CATH significantly reduces the extent of pulmonary fibrin deposition and prevents thrombosis in mice.
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PI3Kα-IN-27
0 ImagesCat. No.: HY-178812CAS No.: 2098649-83-1PI3Kα-IN-27 (Compound 50b) is an orally active PI3K-α inhibitor, with an IC50 of 40 nM. PI3Kα-IN-27 effectively inhibits PAK3, p110α, phospho-mTOR and phospho-ERK1/2. PI3Kα-IN-27 induces early Apoptosis. PI3Kα-IN-27 shows anticancer activity against pancreatic cancer, lung cancer, breast cancer.
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ABC294735
0 ImagesCat. No.: HY-112385CAS No.: 917236-13-6ABC294735 is an orally active SK1/SK2 inhibitor. Combination of ABC294735 with Sorafenib (HY-10201) reduces pERK. ABC294735 exhibits anticancer activity against pancreatic adenocarcinoma and renal cell carcinoma. ABC294735 can be used in research related to pancreatic adenocarcinoma and renal cell carcinoma.
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BRAFV600E/ABL2-IN-2
0 ImagesCat. No.: HY-181726BRAFV600E/ABL2-IN-2 is a dual BRAFV600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma.
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EGFR-IN-181
0 ImagesCat. No.: HY-178939EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases.
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PROTAC SOS1 degrader-10
0 ImagesCat. No.: HY-161654CAS No.: 3043923-74-3PROTAC SOS1 degrader-10 is a SOS1 PROTAC degrader dependent on CRBN and the proteasome. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS-mutant cancer cells SW620, A549 and DLD-1, with DC50 values of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits ERK phosphorylation. PROTAC SOS1 degrader-10 suppresses the proliferation of KRAS-mutant cancer cells via antiproliferative activity. PROTAC SOS1 degrader-10 can be used in studies related to KRAS-mutant cancers.
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Chalcomoracin
0 ImagesCat. No.: HY-N20674CAS No.: 76472-89-4Chalcomoracin is an orally active anticancer agent. Chalcomoracin exhibits anticancer, antibacterial, and α-glucosidase inhibitory activities, with an IC50 of 14.23 µM against yeast α-glucosidase and an IC50 of 5.5 μM against FabI of Staphylococcus aureus. Chalcomoracin reduces the phosphorylation levels of ERK, JNK, and P38; enhances the phosphorylation level of ERK1/2; regulates the MAPK, mTOR, AKT, and p53 signaling pathways; upregulates the expression of Chop, Bip, PINK1, GRP78, and GADD153; and downregulates the expression of Alix. Chalcomoracin induces apoptosis (apoptosis), endoplasmic reticulum stress (endoplasmic reticulum stress), paraptosis (paraptosis), ROS production, mitophagy (mitophagy), and autophagy (autophagy); it inhibits cancer cell viability, colony-forming ability, migration, invasion, proliferation, tumorigenesis, fatty acid synthesis, S. aureus growth, vitreous-stimulated retinal cell activity, and cell cycle progression at the G0/G1 phase. Chalcomoracin can be used in research related to hepatocellular carcinoma, non-small cell lung cancer, triple-negative breast cancer, prostate cancer, proliferative vitreoretinopathy, pancreatic cancer, diabetes, and bacterial infections.
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CSF1R-IN-27
0 ImagesCat. No.: HY-183569CAS No.: 3034296-91-5CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC50 values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury.
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Cyprodinil-d5
0 ImagesCat. No.: HY-116214SCAS No.: 1773496-67-5Synonyms: CGA-219417-d5Cyprodinil-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.
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VEGFR2/C-RAF kinase-IN-1
0 ImagesCat. No.: HY-189471VEGFR2/C-RAF kinase-IN-1 is a type II dual kinase inhibitor targeting VEGFR2 and C-RAF, with IC50 values of 12.22 nM and 38.04 nM, respectively. VEGFR2/C-RAF kinase-IN-1 binds VEGFR2 and CRAF in a Type-II mode and inhibits the downstream Raf-MEK-ERK signaling cascade. VEGFR2/C-RAF kinase-IN-1 induces cell cycle arrest, apoptosis, and intracellular ROS accumulation in H1299 cells, while partially inhibiting P-gp efflux function. VEGFR2/C-RAF kinase-IN-1 can be used for cancer research, such as non-small cell lung cancer and liver cancer.
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BRAFV600E/JNK-IN-1
0 ImagesCat. No.: HY-173153BRAFV600E/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.
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AD-35
0 ImagesCat. No.: HY-117710BCAS No.: 1531586-64-7AD-35 is an orally active, blood-brain barrier-permeable acetylcholinesterase inhibitor with an IC50 of 793 nM. AD-35 inhibits metal-induced amyloid-β aggregation and disassembles preformed amyloid-β aggregates. In rat models of cognitive impairment, AD-35 attenuates Aβ25-35-induced astrocyte activation, TNF-α and IL-1β release, inhibits ERK phosphorylation, and alleviates learning and memory deficits. AD-35 can be used for research on Alzheimer's disease.
