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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEKK (MAP3K)-GNE-3511
GNE-3511

Chemical Structure : GNE-3511

CAS No.: 1496581-76-0

GNE-3511 (GNE3511, GNE 3511)

货号: PC-43286Not For Human Use, Lab Use Only.

GNE-3511 is a potent, selective, orally bioavailable, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of <0.5 nM, displays >100-fold selectivity over MKK4/7, JNK1/2/3, MLK1/2/3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GNE-3511 (GNE3511) is a potent, selective, orally bioavailable, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of <0.5 nM, displays >100-fold selectivity over MKK4/7, JNK1/2/3, MLK1/2/3.
GNE-3511 also shows high affinity with Kd of 8.9 nM for leucine zipper-bearing kinase (LZK, MAP3K13).
GNE-3511 inhibits p-JNK with IC50 of 30 nM, displays concentration-dependent protection of neurons from degeneration in vitro (DRG IC50=107 nM).
GNE-3511 demonstrates dose-dependent activity in multiple animal models of neurodegenerative disease.

物理化学性质&存储条件

分子量 440.489
分子式 C23H26F2N6O
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

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

4-Pyridinecarbonitrile, 2-[[6-(3,3-difluoro-1-pyrrolidinyl)-4-[1-(3-oxetanyl)-4-piperidinyl]-2-pyridinyl]amino]-

参考文献

1. Patel S, et al. J Med Chem. 2015 Jan 8;58(1):401-18.

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