MK-28 |
Katalog-Nr.GC61072
One-Click Copy Product Info
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MK-28 ist ein potenter und selektiver PERK-Aktivator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 864388-65-8
Sample solution is provided at 25 µL, 10mM.
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MK-28 is a potent and selective agonist of pancreatic endoplasmic reticulum kinase (PERK), which functions by modulating the endoplasmic reticulum stress response[1]. MK-28 exhibits favorable pharmacokinetic properties and has the ability to cross the blood-brain barrier[2]. MK-28 has been shown to improve motor and executive function, as well as effectively extend the survival period, in a Huntington's disease mouse model[3].
In vitro, pretreatment of STHdhQ111/111 striatal cells (a Huntington's disease model) with MK-28 (5-100μM) for 48 hours significantly reduced endoplasmic reticulum stress-induced apoptosis, while concurrently increasing the levels of eIF2α phosphorylation and ATF4 protein expression[2].
In vivo, administration of MK-28 (0.3-1mg/kg) via intraperitoneal injection three times per week, starting from 3 weeks of age in R6/2 Huntington's disease model mice, significantly ameliorated motor dysfunction and extended their survival[3].
References:
[1] Costa MFD, Höglinger GU, Rösler TW. Development of a cell-free screening assay for the identification of direct PERK activators. PLoS One. 2023 May 18;18(5):e0283943.
[2] Ganz J, Shacham T, Kramer M, et al. A novel specific PERK activator reduces toxicity and extends survival in Huntington's disease models. Sci Rep. 2020 Apr 23;10(1):6875.
[3] Shacham T, Offen D, Lederkremer GZ. Efficacy of therapy by MK-28 PERK activation in the Huntington's disease R6/2 mouse model. Neurotherapeutics. 2024 Mar;21(2):e00335.
| Cell experiment [1]: | |
Cell lines | STHdhQ111/111 cells (murine striatal cell line expressing full-length polyQ-expanded mutant huntingtin) |
Preparation Method | STHdhQ111/111 cells were incubated with the ER stress-inducer tunicamycin (Tun) and in parallel with increasing concentrations of MK-28 (5-100μM). Apoptosis was measured after 48h of Tun exposure. |
Reaction Conditions | 5-100μM; 48 hours |
Applications | MK-28 strongly protected cells from ER stress-induced apoptosis in a dose-dependent manner, reducing apoptosis by 5-fold at 100μM. |
| Animal experiment [2]: | |
Animal models | B6CBA R6/2 Huntington's disease model mice |
Preparation Method | Mice were treated from the age of 3 weeks by intraperitoneal injection 3 times a week with different doses of MK-28 (0.1, 1, and 10mg/kg). Body weight and blood glucose levels were monitored weekly. |
Dosage form | 0.1, 1, and 10mg/kg; i.p. |
Applications | MK-28 showed a positive influence on body weight, significantly slowing down weight loss at 1mg/kg at 12 weeks of age. Blood glucose levels, which were significantly increased in Huntington's disease mice, returned to regular levels or slightly below in all treated groups at 8 weeks of age. |
References: | |
| Cas No. | 864388-65-8 | SDF | |
| Canonical SMILES | OC1=CC=C(C=C1O)/C=N/N(C2=NC(C3=CC=CC=C3)=CC(C4=CC=CC=C4)=N2)C | ||
| Formula | C24H20N4O2 | M.Wt | 396.44 |
| Löslichkeit | DMSO: 12.5 mg/mL (31.53 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL |
| 5 mM | 504.5 μL | 2.5224 mL | 5.0449 mL |
| 10 mM | 252.2 μL | 1.2612 mL | 2.5224 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)