1. Cell Cycle/DNA Damage
  2. PERK
  3. MK-28

MK-28 

Cat. No.: HY-137207
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MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.

For research use only. We do not sell to patients.

MK-28 Chemical Structure

MK-28 Chemical Structure

CAS No. : 864388-65-8

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Description

MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1].

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[1].
ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ111/111 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[1].
MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2)[1].

Apoptosis Analysis[1].

Cell Line: STHdhQ111/111 cells.
Concentration: 0-100 μM.
Incubation Time: 48 h.
Result: Rescued cells from ER stress-induced apoptosis.
In Vivo

MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (Cmax) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection[1].
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[1].
MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity[1].

Animal Model: R6/2 mice[1].
Dosage: 1 mg/kg.
Administration: IP, daily for 28 days.
Result: Incerased the survival.
Molecular Weight

396.44

Formula

C₂₄H₂₀N₄O₂

CAS No.

864388-65-8

SMILES

OC1=CC=C(C=C1O)/C=N/N(C2=NC(C3=CC=CC=C3)=CC(C4=CC=CC=C4)=N2)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MK-28MK28MK 28PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseHuntingtonER-stressInhibitorinhibitorinhibit

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MK-28
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