中文名 | Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone |
英文名 | Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone |
英文别名 | MK-28 Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone |
CAS | 864388-65-8 |
化学式 | C24H20N4O2 |
分子量 | 396.44 |
密度 | 1.22±0.1 g/cm3(Predicted) |
沸点 | 658.4±65.0 °C(Predicted) |
酸度系数 | 8.35±0.35(Predicted) |
体外研究 | 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. |
体内研究 | 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. |
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