化合物 MK-28
| 中文名称 | 化合物 MK-28 |
|---|---|
| 中文同义词 | 化合物 MK-28;4-((2-(4,6-二苯基嘧啶-2-基)-2-甲基亚肼基)甲基)苯-1,2-二酚 |
| 英文名称 | Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone |
| 英文同义词 | Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone;MK-28;4-((2-(4,6-Diphenylpyrimidin-2-yl)-2-methylhydrazineylidene)methyl)benzene-1,2-diol , MK-28;4-((2-(4,6-Diphenylpyrimidin-2-yl)-2-methylhydrazineylidene)methyl)benzene-1,2-diol |
| CAS号 | 864388-65-8 |
| 分子式 | C24H20N4O2 |
| 分子量 | 396.44 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 864388-65-8.mol |
| 结构式 |  |
化合物 MK-28 性质
| 沸点 | 658.4±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：12.5 mg/mL（31.53 mM） |
| 酸度系数(pKa) | 8.35±0.35(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
| 水溶解性 | Water: < 0.1 mg/mL (insoluble) |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-137207 | MK-28 | 1 mg | 1364元 | |
| 2024/08/19 | HY-137207 | MK-28 | 864388-65-8 | 5mg | 3000元 |