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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CAF-382
CAF-382

Chemical Structure : CAF-382

CAS No.:

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CAF-382 (CDKL5 inhibitor B1, CAF382, SGC-CAF382-1)

货号: PC-20880Not For Human Use, Lab Use Only.

CAF-382 (SGC-CAF382-1) is a potent, specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) with IC50 of 11 nM in NanoBRET assays, shows no activity against GSK3β.

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

    生物&药学活性

    CAF-382 (SGC-CAF382-1) is a potent, specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) with IC50 of 11 nM in NanoBRET assays, shows no activity against GSK3β.
    CAF-382 shows high CDKL5 affinity in CDKL5 split-luciferase assays with IC50 of 6.7 nM, does not inhibit CDKL2 at 10 uM.
    CAF-382 has a good selectivity score (S10 (1 µM)=0.017) in the DiscoverX scanMAX panel, several CDKs (CDK9, PCTK1/CDK16, PCTK2/CDK17, PCTK3/CDK18) are potently inhibited (IC50 ≤100 nM).
    CAF-382 (5 nM) caused a significant reduction in pSer222 EB2 without a change in total EB2 levels in rat primary cortical neuron cultures.
    CAF-382 (100 nM) reduces EB2 phosphorylation in a dose dependent fashion in rat hippocampal slices, selectively reduces AMPA-type glutamate receptor-mediated responses post-synaptically.
    CAF-382 reduces hippocampal long-term potentiation (LTP).

    物理化学性质&存储条件

    分子量 366.50
    分子式 C16H22N4O2S2
    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

    N-(5-(((5-isopropyloxazol-2-yl)methyl)thio)thiazol-2-yl)piperidine-4-carboxamide

    参考文献

    1. Castano A, et al. bioRxiv. 2023 Apr 24:2023.04.24.538049.

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