PERK
Os inibidores de PERK (Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase) têm como alvo a via PERK, que está envolvida na resposta celular ao estresse do retículo endoplasmático (ER) e na regulação da apoptose. PERK desempenha um papel crítico na resposta a proteínas mal enoveladas (UPR), interrompendo a tradução de proteínas e promovendo a sobrevivência celular sob condições de estresse. No entanto, a ativação prolongada de PERK pode levar à apoptose. A inibição de PERK pode modular essas respostas ao estresse, tornando esses inibidores valiosos na pesquisa de doenças neurodegenerativas, câncer e distúrbios metabólicos. Na CymitQuimica, oferecemos uma gama de inibidores de PERK de alta qualidade para apoiar sua pesquisa em apoptose, estresse do RE e homeostase celular.
Foram encontrados 34 produtos para "PERK".
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GCN2-IN-6
CAS:GCN2-IN-6: Potent, oral GCN2/PERK inhibitor; IC50s - GCN2: 1.8 nM (enzymatic), 9.3 nM (cellular); PERK: 0.26 nM (enzymatic), 230 nM (cellular).Fórmula:C19H12Cl2F2N4O3SPureza:95.04% - 98.72%Cor e Forma:Yellow SolidPeso molecular:485.291HC-5404-Fu
CAS:HC-5404-Fu is an inhibitor of PERK with anti-tumor activity. This compound inhibits the signaling pathway of the endoplasmic reticulum stress response. Additionally, HC-5404-Fu increases the sensitivity of renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). It holds potential for research into renal cell carcinoma, stomach cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.Fórmula:C28H28F2N4O7Cor e Forma:SolidPeso molecular:570.54eIF4A-IN-1
CAS:eIF4A-IN-1 is an eIF4A inhibitor used in tumor research.Fórmula:C31H33N3O5Cor e Forma:SolidPeso molecular:527.61HC-7366
CAS:HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.Fórmula:C20H15ClF2N6O4SPureza:99.84%Cor e Forma:White SolidPeso molecular:508.89HR-19011
CAS:HR-19011 (Compound 40) is an inducer of eIF2α phosphorylation that increases expression levels of downstream proteins ATF and CHOP,antiproliferative.Fórmula:C25H19F6N3O3Pureza:99.89%Cor e Forma:Yellow SolidPeso molecular:523.43RAPT-37-Me
CAS:RAPT-37-Me is a GCN2 inhibitor, exhibiting IC50 values for GCN2, PERK, HRl, and PKR of 0.002 μM, >10 μM, 4.40 μM, and 1.31 μM, respectively.Fórmula:C22H21BrFN7OPeso molecular:498.36eIF4E-IN-4
CAS:eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.Fórmula:C20H19ClN5O5PCor e Forma:SolidPeso molecular:475.822GCN2 activator-1
CAS:GCN2 activator-1 (Compound 20) is a GCN2 activator that binds to the ATP pocket of GCN2 and activates it in a GCN1-independent manner. It can stimulate the integrated stress response (ISR) in cells and inhibits PKR with an IC50 of 3.75 µM. GCN2 activator-1 is utilized for research on pulmonary veno-occlusive disease (PVOD).Fórmula:C11H10N6S2Peso molecular:290.3671,3-Bis[3,5-bis(trifluoromethyl)phenyl]urea
CAS:1,3-Bis[3,5-bis(trifluoromethyl)phenyl]urea effectively activates the heme-regulated inhibitor of eIF2α kinase. It reduces the abundance of the eIF2·GTP·tRNAiMet ternary complex and can inhibit the proliferation of cancer cells.Fórmula:C17H8F12N2OPeso molecular:484.2391KRAS-IN-56
CAS:KRAS-IN-56 (Compound 18) is a KRAS inhibitor with an EC50 of 33 μM. It disrupts the interaction between GTP-KRAS and SOS1, and reduces p-ERK levels. KRAS-IN-56 is applicable for research related to lung cancer.Fórmula:C19H19N3O2Peso molecular:321.37NCATS-SM0225
CAS:NCATS-SM0225 is an ER-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2, and VDAC3. It has an IC50 of 1.02 μM for ERAD inhibition and a Kd of 3.13 μM for binding to human VDAC1. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling, and activates PERK. The compound selectively kills cancer cells and has shown tumor growth inhibition in melanoma xenograft models. It is useful for research into various cancers, including melanoma, as well as studies on ERAD and calcium homeostasis regulatory mechanisms.Fórmula:C23H28N2O4S2Peso molecular:460.61ISR activator 3
CAS:ISR activator 3 (Compound cc81) is the active metabolite of A8. It activates the integrated stress response (ISR) by binding to RIG-I (KD≈ 0.55 μM) without inducing lipid droplet clearance. Additionally, ISR activator 3 enhances the interferon response under viral mimic signaling. This compound is applicable in studies of neurodegenerative diseases and immune stress.Fórmula:C23H21N3O3S2Peso molecular:451.56APL-4098
CAS:APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. It reduces the phosphorylation levels of eIF2α and the expression of ATF4. APL-4098 impairs mitochondrial function and exhibits cytotoxicity against primary acute myeloid leukemia cells. It is applicable in studies related to acute myeloid leukemia.Fórmula:C17H12ClFN6O3SPeso molecular:434.83HC-5404
CAS:HC-5404 is a potent and selective PERK inhibitor, blocking the activation of the PERK pathway, anti-tumor effects, advanced solid tumors and renal cell Cancer.Fórmula:C24H24F2N4O3Pureza:99.33%Cor e Forma:White SolidPeso molecular:454.47
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