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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-GSK-3-LY2090314
LY2090314

Chemical Structure : LY2090314

CAS No.: 603288-22-8

LY2090314 (LY 2090314)

货号: PC-20193Not For Human Use, Lab Use Only.

LY2090314 is a potent and selective ATP-competitive inhibitor of Glycogen synthase kinase-3 (GSK-3) with IC50 of 1.5/0.9 nM for GSK3α/GSK3β, respectively.

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10 mg ¥1480 In stock
25 mg ¥2580 In stock
50 mg ¥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LY2090314 is a potent and selective ATP-competitive inhibitor of Glycogen synthase kinase-3 (GSK-3) with IC50 of 1.5/0.9 nM for GSK3α/GSK3β, respectively.
LY2090314 stimulated TCF/LEF TOPFlash reporter activity, stabilized β-catenin and elevated the expression of Axin2 in a panel of melanoma cell lines at nM potency.
LY2090314 exhibited cytotoxicity against melanoma cell lines in vitro with IC50 of 10 nM, but not other solid tumor cell lines (IC50 >10 uM).
LY2090314 elevates Axin2 gene expression after a single dose and produces tumor growth delay in A375 melanoma xenografts with repeat dosing.

物理化学性质&存储条件

分子量 512.55
分子式 C28H25FN6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[9-fluoro-2-(piperidin-1-ylcarbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-4-imidazo[1,2-a]pyridin-3-yl-1H-pyrrole-2,5-dione

参考文献

1. Atkinson JM, et al. PLoS One. 2015 Apr 27;10(4):e0125028.

2. Rizzieri DA, et al. Leuk Lymphoma. 2016 Aug;57(8):1800-6.

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