MK-28
Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone
CAS: 864388-65-8
Molecular Formula: C24H20N4O2
MK-28 - Names and Identifiers
| Name | Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone |
| Synonyms | MK-28 Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone |
| CAS | 864388-65-8 |
MK-28 - Physico-chemical Properties
| Molecular Formula | C24H20N4O2 |
| Molar Mass | 396.44 |
| Density | 1.22±0.1 g/cm3(Predicted) |
| Boling Point | 658.4±65.0 °C(Predicted) |
| pKa | 8.35±0.35(Predicted) |
| In vitro study | 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. |
| In vivo study | 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. |
MK-28 - Reference Information
| biological activity | MK-28 are effective and selective PERK agonists. MK-28 showed good pharmacokinetic characteristics in mice and could penetrate the blood-brain barrier. |
| in vitro study | MK-28 (0-100μ m) 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: 0-100μM. Incubation Time: 48 h. Result: Rescued cells from ER stress-induced apoptosis. |
| Cell Line: | ST Hdh Q 111/111 cells. |
| Concentration: | 0-100 μM. |
| Incubation Time: | 48 h. |
| Result: | Rescued cells from ER stress-induced apoptosis. Incerased the survival. |
| in vivo study | 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 after 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. |
| Animal Model: | R6/2 mice. |
| Dosage: | 1 mg/kg. |
| Administration: | IP, daily for 28 days. |
Last Update：2024-04-09 21:01:54
