MK-28 is a potent selective PERK activator. In terms of saving striatal neurons expressing mutated Huntington protein (mHtt) from apoptosis, the IC50 of MK-28 was about 3 times higher than that of CCT020312. MK-28 showed significant pharmacokinetic properties and high BBB permeability in mice.

 

Brand: BCM

 

In Vitro: 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.

 

Boiling Point: 658.4±65.0 °C(Predicted)

 

pKa: 8.35±0.35(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

Isomeric SMILES: CN(C1=NC(=CC(=N1)C2=CC=CC=C2)C3=CC=CC=C3)/N=C\C4=CC(=C(C=C4)O)O  

 

InChIKey: GKOVHCFOVLXKFL-XYGWBWBKSA-N  

 

InChI: 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-

 

Attribute
[Chem Name]	4-[(Z)-[(4,6-diphenylpyrimidin-2-yl)-methylhydrazinylidene]methyl]benzene-1,2-diol
[Synonym]	MK-28
[CAS No.]	864388-65-8
[MDL No.]	MFCD32874143
[Formula]	C24H20N4O2
[Molecular]	396.44
[Form]	Solid powder
[Storage]	Sealed in dry. Stored at -20°C.

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