864388-65-8
864388-65-8 結(jié)構(gòu)式
基本信息
Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone
物理化學(xué)性質(zhì)
常見問題列表
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).
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. |
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.
| Animal Model: |
R6/2 mice.
|
| Dosage: | 1 mg/kg. |
| Administration: | IP, daily for 28 days. |
| Result: | Incerased the survival. |