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 (203)
Related Products (203)
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Antibodies (2)
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ONO-8130
0 ImagesCat. No.: HY-110198CAS No.: 459841-96-4
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PROTAC SOS1 degrader-1
0 ImagesCat. No.: HY-145737CAS No.: 2913185-35-8PROTAC SOS1 degrader-1 is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers.
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Milnacipran-d5 hydrochloride
0 ImagesCat. No.: HY-B0168ASCAS No.: 2750534-79-1Milnacipran-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).
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CYB-5067
0 ImagesCat. No.: HY-184598CYB-5067 is a FGFR molecular glue degrader with a DC50 of 27 nM against FGFR2. CYB-5067 inhibits FGFR1, FGFR3, FGFR4 and downstream FGFR signaling pathways, induces antiproliferative activity in vitro, and exhibits sustained target protein inhibition in vivo without obvious hook effect. CYB-5067 shows significant tumor growth inhibitory activity in the ETV6-FGFR2 fusion Ba/F3 xenograft model. CYB-5067 can be used for the research of FGFR-driven cancers.
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Cyanidin 3,5-diglucoside chloride (Standard)
0 ImagesCat. No.: HY-129138RCAS No.: 2611-67-8Cyanidin 3,5-diglucoside (chloride) (Standard) is the analytical standard of Cyanidin 3,5-diglucoside (chloride) (HY-129138). This product is intended for research and analytical applications. 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.
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BRAFV600E/ABL2-IN-1
0 ImagesCat. No.: HY-178382BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma.
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Pulegone-d8
0 ImagesCat. No.: HY-N1500S1CAS No.: 62385-90-4Pulegone-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.
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DPAP
0 ImagesCat. No.: HY-182899DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma.
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(Rac)-8-Gingerol
0 ImagesCat. No.: HY-N16557CAS No.: 77398-92-6(Rac)-8-Gingerol is a non-volatile component. (Rac)-8-Gingerol can be extracted from ginger. (Rac)-8-Gingerol enhances Apoptosis. (Rac)-8-Gingerol decreases the level of phosphorylated EGFR and, accordingly, the phosphorylation levels of its downstream effectors, STAT3 and ERK. (Rac)-8-Gingerol exhibits anticancer activity against colorectal cancer.
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KRAS-IN-54
0 ImagesCat. No.: HY-181704CAS No.: 3084918-70-4KRAS-IN-54 is a macrocyclic KRAS inhibitor. KRAS-IN-54 exhibits activity against cell viability and pERK inhibition in cells with KRASG12D and KRASG13D mutations. KRAS-IN-54 can be used in the research of KRAS-mutant cancers, including pancreatic adenocarcinoma, colorectal cancer, non-small cell lung cancer, esophageal cancer, gallbladder cancer, melanoma, ovarian cancer and endometrial cancer.
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α-Neoendorphin (porcine)
0 ImagesCat. No.: HY-P11656CAS No.: 77739-20-9α-Neoendorphin porcine is a peptide. α-Neoendorphin porcine effectively alleviates UVB-induced skin photoaging via activating mTOR-Beclin-1-mediated autophagy, reducing UVB-triggered ROS production, inhibiting the MAPK pathway and MMP activity, and promoting type I procollagen synthesis. α-Neoendorphin porcine exerts anti-aging and anti-wrinkle effects on skin cells. α-Neoendorphin porcine can be used in studies related to skin photoaging.
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YN14 (mixture of diastereomers)
0 ImagesCat. No.: HY-155356ACAS No.: 3053689-54-3YN14 mixture of diastereomers is a diastereomer mixture of YN14 (HY-155356). YN14 is a KRASG12C PROTAC degrader that recruits E3 ubiquitin ligase to induce the polyubiquitination and proteasomal degradation of KRASG12C. YN14 induces tumor cell apoptosis, cell cycle arrest, and cell migration inhibition. YN14 exhibits in vivo antitumor proliferative activity in tumor cell xenograft nude mice. YN14 can be used in cancer-related research.
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HDAC6-IN-74
0 ImagesCat. No.: HY-181579HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.
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L-Azetidine-2-carboxylic acid (Standard)
0 ImagesL-Azetidine-2-carboxylic acid is a proline analog. L-Azetidine-2-carboxylic acid upregulates the lipid autophagy marker LC3-II via activation of the PERK pathway. L-Azetidine-2-carboxylic acid increases pro-apoptotic BAX protein. L-Azetidine-2-carboxylic acid induces ATF6 cleavage and upregulates phosphorylated eIF2α levels. L-Azetidine-2-carboxylic acid induces ER stress, inducing protein misfolding and aggregation. L-Azetidine-2-carboxylic acid shows teratogenic, pro-inflammatory and pro-apoptotic effects.
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6-Methoxyflavone (Standard)
0 ImagesCat. No.: HY-W097625RCAS No.: 26964-24-96-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases.
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DGAT-1 inhibitor 2 (Standard)
0 ImagesCat. No.: HY-50670RCAS No.: 942999-61-3DGAT-1 inhibitor 2 (Standard) is the analytical standard of DGAT-1 inhibitor 2 (HY-50670). This product is intended for research and analytical applications. 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.
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Benzoylpaeoniflorin (Standard)
0 ImagesCat. No.: HY-N0852RCAS No.: 38642-49-8Benzoylpaeoniflorin (Standard) is an analytical standard for Benzoylpaeoniflorin (HY-N0852). This product is intended for research and analytical applications. Benzoylpaeoniflorin is an orally active monoterpene glycoside compound. Benzoylpaeoniflorin exerts anti-inflammatory, anti-allergic, psoriasis-improving and sepsis-improving effects by inhibiting signaling pathways such as TNF/NF-κB and MAPK, as well as regulating immune homeostasis. Benzoylpaeoniflorin can be used in research related to immune, allergic and inflammatory diseases.
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ML291 (Standard)
0 ImagesCat. No.: HY-101991RCAS No.: 1523437-16-2ML291 (Standard) is the analytical standard of ML291 (HY-101991). This product is intended for research and analytical applications. 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.
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Lard oil
0 ImagesCat. No.: HY-W127601CAS No.: 8016-28-2Lard oil is an orally active biochemical reagent. Lard oil upregulates PERK, eIF2a, CHOP, OPN, TLR2, TLR4, TNF-α, and downregulates GRP78 and IRE1a. Lard oil induces responses such as body fat accumulation, elevated serum insulin levels, increased HOMA-IR, hepatic ectopic lipid deposition, hepatic endoplasmic reticulum stress, and hepatic inflammation. Lard oil can be used in studies related to diet-induced obesity, insulin resistance, and non-alcoholic fatty liver disease.
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Dehydrodiisoeugenol (Standard)
0 ImagesDehydrodiisoeugenol (Standard) is the analytical standard of Dehydrodiisoeugenol (HY-N0589). This product is intended for research and analytical applications. 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.
