MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
In Vitro
MK-28 (0-100 μM) shows PERK selectivity in vitro on a 391-kinase panel and rescues cells (but not PERK −/− cells) from ER stress-induced apoptosis. ATF4 protein levels are increased signifcantly, up to 2.5-fold, in ST Hdh Q 111/111 cells at high MK-28 concentration. CHOP and GADD34 mRNA levels show a signifcant increase in both cell types, up to 10- and 5-fold respectively. MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis Analysis. Cell Line: ST Hdh Q 111/111 cells. Concentration: 0-100 μM. Incubation Time: 48 h. Result: Rescued cells from ER stress-induced apoptosis.
In Vivo
MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (C max ) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection . MK-28 (1 mg/kg, IP, daily for 28 days) improves systemic function and survival in R6/2 mice and induces increased levels of eIF2α-P in the mouse brain striatum . MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: R6/2 mice . Dosage: 1 mg/kg. Administration: IP, daily for 28 days. Result: Incerased the survival.
Form:Solid
Especificaciones
Especificaciones y pureza
≥99%
Mecanismos bioquímicos y fisiológicos
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
Condiciones de almacenamiento de almacenamiento
Store at -20°C
Enviado en
Ice chest + Ice pads
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Tipo de acción
ACTIVATOR
Pureza
≥99%
Nombres e identificadores
Peso molecular
396.44
Datos avanzados
Certificados (CoA, COO, BSE/TSE y tabla de análisis)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propiedades químicas y físicas
Solubilidad
DMSO : 12.5 mg/mL (31.53 mM; Need ultrasonic)
Calculadoras de soluciones
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
Utilizamos cookies para garantizar el correcto funcionamiento del sitio web y, cuando esté permitido, para mejorar su experiencia. Puede gestionar sus preferencias en cualquier momento en Configuración. Más información en nuestra Política de Cookies.
¿Quieres que te enviemos un mensaje cuando tengamos descuentos disponibles?
Recordármelo más tarde
¡Gracias! Por favor, revisa tu bandeja de entrada de correo electrónico para confirmar.
Products are supplied to verified businesses, institutions, and qualified professionals for research and development use only. Not for use in humans, animals, diagnosis, or therapy.