MK-28,864388-65-8

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MK-28

CAS No. : 864388-65-8

MCE 国际站：MK-28

产品活性：MK-28 是有效、选择性的 PERK 激动剂。MK-28 在小鼠中表现出良好的药代动力学特征，且能透过血脑屏障。

研究领域：Cell Cycle/DNA Damage

作用靶点：PERK

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 STHdhQ^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).

In Vivo: 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.

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