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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEKK (MAP3K)-IACS-52825
IACS-52825

Chemical Structure : IACS-52825

CAS No.: 2640376-72-1

IACS-52825 (IACS52825, IACS 52825)

货号: PC-20983Not For Human Use, Lab Use Only.

IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.

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

    生物&药学活性

    IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.
    IACS-52825 shows no significant inhibition of the hERG channel or CYP P450 enzymes and no significant activities against an 80-member Eurofins CEREP panel of various ion channels and receptors or a 403-member Eurofins DiscoverX kinase panel.
    IACS-52825 (orally once daily at 3, 10, or 30 mg/kg) dose-dependently reverses cisplatin-induced mechanical allodynia.

    物理化学性质&存储条件

    分子量 426.29
    分子式 C16H13F7N4O2
    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

    (R)-1-(4-(6-Amino-5-(trifluoromethoxy)pyridin-3-yl)-1-(3-fluorobicyclo[1.1.1]pentan-1-yl)-1H-imidazol-2-yl)-2,2,2-trifluoroethanol

    参考文献

    1. Kang Le, et al. J Med Chem. 2023 Jul 12. doi: 10.1021/acs.jmedchem.3c00788.

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