864388-65-8
864388-65-8 structure
- Name: MK-28
- Chemical Name: MK-28
- CAS Number: 864388-65-8
- Molecular Formula: C24H20N4O2
- Molecular Weight: 396.44
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PERK
- Create Date: 2020-10-21 07:20:13
- Modify Date: 2024-01-05 12:46:38
-
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1].
| Name | MK-28 |
|---|
| Description | MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1]. |
|---|---|
| Related Catalog | |
| 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[1]. ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ111/111 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[1]. MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2)[1]. Apoptosis Analysis[1]. Cell Line: STHdhQ111/111 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 (Cmax) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection[1]. 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[1]. MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity[1]. Animal Model: R6/2 mice[1]. Dosage: 1 mg/kg. Administration: IP, daily for 28 days. Result: Incerased the survival. |
| References |
| Molecular Formula | C24H20N4O2 |
|---|---|
| Molecular Weight | 396.44 |