| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
MK-28 (0-100 μM) rescues cells from ER stress-induced apoptosis and demonstrates PERK selectivity in vitro on a 391-kinase panel (but not PERK−/− cells)[1]. When MK-28 concentrations are high, ATF4 protein levels in STHdhQ111/111 cells grow significantly—up to a 2.5-fold increase. Both cell types exhibit a significant rise in CHOP and GADD34 mRNA levels, up to 10- and 5-fold, respectively[1]. MK-28 activates EIF2AK4 (GCN2) but has little or no effect on EIF2AK1 (HRI) or EIF2AK2 (PKR)[1].
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|---|---|
| ln Vivo |
MK-28 (10 mg/kg, IP, single dose) exhibits a 40-minute half-life in plasma and a maximal concentration (Cmax) of 105 ng/ml[1]. MK-28 (1 mg/kg, IP, daily for 28 days) increases eIF2α-P levels in the mouse brain striatum and enhances survival and systemic function in R6/2 mice[1]. In R6/2 mice, MK-28 (transient subcutaneous administration) exhibits no toxicity and considerably enhances motor and executive functions as well as delaying the start of death[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: STHdhQ111/111 cells. Tested Concentrations: 0-100 μM. Incubation Duration: 48 h. Experimental Results: Rescued cells from ER stress-induced apoptosis. |
| Animal Protocol |
Animal/Disease Models: R6/2 mice[1].
Doses: 1 mg/ kg. Route of Administration: IP, daily for 28 days. Experimental Results: Incerased the survival. |
| References |
| Molecular Formula |
C24H20N4O2
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|---|---|
| Molecular Weight |
396.44
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| Exact Mass |
396.158
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| CAS # |
864388-65-8
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| PubChem CID |
135425028
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
521
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C=CC(C2=NC(N(/N=C/C3=CC(=C(C=C3)O)O)C)=NC(C3C=CC=CC=3)=C2)=CC=1
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| InChi Key |
GKOVHCFOVLXKFL-XYGWBWBKSA-N
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| InChi Code |
InChI=1S/C24H20N4O2/c1-28(25-16-17-12-13-22(29)23(30)14-17)24-26-20(18-8-4-2-5-9-18)15-21(27-24)19-10-6-3-7-11-19/h2-16,29-30H,1H3/b25-16-
|
| Chemical Name |
4-[(Z)-[(4,6-diphenylpyrimidin-2-yl)-methylhydrazinylidene]methyl]benzene-1,2-diol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 12.5 mg/mL (31.53 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.15 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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