GSK2578215A

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

GSK2578215A 是一种高效、选择性、BBB 可渗透的 LRRK2 抑制剂，对野生型 LRRK2 和 G2019S 突变体的 IC50 分别为 10.9 和 9.9 nM。

GSK2578215A is a highly potent, selective, BBB-permeable LRRK2 inhibitor with IC50 of 10.9 and 9.9 nM for wild-type LRRK2 and the G2019S mutant, respectively; shows 8-fold reduced potentcy against A2016T mutant LRRK2 (IC50=81 nM); inhibits Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 G2019S stably transfected into HEK293 cells at 0.1-0.3 uM, also induces dephosphorylation of Ser910 and 935 at 1-3 μM in the inhibitor-resistant LRRK2[A2016T+ G2019S] and LRRK2 [A2016T] mutants; induces protective autophagy in SH-SY5Y cells.

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Animal Model:mice bearing OVCAR8 xenografts Dosage:5 mg/kg, with Olaparib (50?mg/kg) Administration:i.p., for 3 weeks Result:Inhibited the tumor growth and increased DNA damage in tumors more potently than Olaparib or GSK2578215A alone.

GSK-2578215A

Autophagy

LRRK2

LRRK2(G2019S)|LRRK2(WT)

Neurological Disease

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1285515-21-0

399.417

C24H18FN3O2

>98% (HPLC)

10 mM in DMSO

O=C(NC1=CC=CN=C1)C2=CC(C3=CC(F)=NC=C3)=CC=C2OCC4=CC=CC=C4

Benzamide, 5-(2-fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-

(-20℃)

With Ice Pack

≥ 2 years