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.
Spécifications
Spécifications et pureté
10mM in DMSO
Mécanismes biochimiques et physiologiques
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
Conditions de stockage de stockage
Store at -80°C
Expédié en
Dry ice packs + Cold packs
Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.
Type d'action
ACTIVATOR
Noms et identifiants
Poids moléculaire
396.44
Données avancées
Certificats (CoA, COO, BSE/TSE et tableau d'analyse)
C of A & Other Certificates(BSE/TSE, COO):
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Foire aux questions
How should this product be stored?
Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.
How is this product shipped?
This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 864388-65-8, the molecular formula is C24H20N4O2, and the molecular weight is 396.44 g/mol.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
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