MK-28

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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

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 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.MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2).Apoptosis Analysis.Cell Line:STHdhQ111/111 cells.Concentration:0-100 μM.Incubation Time:48 h.Result:Rescued cells from ER stress-induced apoptosis.

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

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Apoptosis

PERK

PERK | Antiviral

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864388-65-8

396.44

C24H20N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 12.5 mg/mL (31.53 mM; 超声助溶 )

CN(\N=C\c1ccc(O)c(O)c1)c1nc(cc(n1)-c1ccccc1)-c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years