864388-65-8
基本信息
Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone
物理化学性质
| 沸点 | 658.4±65.0 °C(Predicted) |
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMSO: 12.5 mg/mL (31.53 mM) |
| 酸度系数(pKa) | 8.35±0.35(Predicted) |
| 形态 | Solid |
| 颜色 | Light yellow to yellow |
| 水溶解性 | Water: < 0.1 mg/mL (insoluble) |
常见问题列表
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. |