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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-SGC-CDKL5/GSK3-1
SGC-CDKL5/GSK3-1

Chemical Structure : SGC-CDKL5/GSK3-1

CAS No.: 844442-32-6

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SGC-CDKL5/GSK3-1 (CDKL5/GSK3 inhibitor 2)

货号: PC-49792Not For Human Use, Lab Use Only.

CDKL5/GSK3 inhibitor 2 is a highly potent and cell-active chemical probe inhibitor of cyclindependent kinase-like 5 (CDKL5)/GSK3 (glycogen synthase kinase 3) with IC50 of 4.6/9.5/24 nM for CDKL5/GSK3⍺/GSK3β, respectively.

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

    生物&药学活性

    SGC-CDKL5/GSK3-1 is a highly potent and cell-active chemical probe inhibitor of cyclindependent kinase-like 5 (CDKL5)/GSK3 (glycogen synthase kinase 3) with IC50 of 4.6/9.5/24 nM for CDKL5/GSK3⍺/GSK3β, respectively.
    SGC-CDKL5/GSK3-1 displays exquisitely selectivity against CDKL family (CDKL1/2/3) and the Eurofins DiscoverX scanMAX panel including 403 wild-type (WT) human as well as several mutant and non-human kinases.
    SGC-CDKL5/GSK3-1 potently inhibits CDKL5 kinase activity and downstream signaling, demonstrates canonical ATP-competitive binding to CDKL5.
    SGC-CDKL5/GSK3-1 (5 nM) inhibits phosphorylation of EB2 and phospho-β-catenin in DIV15-16 cortical primary rat neurons.
    SGC-CDKL5/GSK3-1 promotes survival of motor neurons in response to ER stress, which is a hallmark of neurodegenerative diseases like ALS.

    物理化学性质&存储条件

    分子量 349.34
    分子式 C16H17F2N5O2
    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

    4-(3,5-difluorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide

    参考文献

    1. Ong HW, et al. bioRxiv. 2023 Feb 10:2023.02.09.527935.

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