1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  3. Casein Kinase

Casein Kinase (酪蛋白激酶)

酪蛋白激酶 (CK) 是一组普遍存在的丝氨酸/苏氨酸激酶,可调节真核生物的多种细胞功能,包括对通过泛素-蛋白酶体系统 (UPS) 降解的底物蛋白质进行磷酸化。已从多种来源鉴定出两种酪蛋白激酶,即酪蛋白激酶-1 (CK-1) 和酪蛋白激酶-2 (CK-2)。

CK1 激酶在哺乳动物中至少有七种亚型 (α、β、γ1-3、δ 和 ɛ),CK1 激酶磷酸化各种底物,在 DNA 修复、细胞周期进程、胞质分裂、分化和细胞凋亡等多种生理过程中发挥重要作用。酪蛋白激酶 2 (CK2) 是一种高度多效性的丝氨酸-苏氨酸激酶,可催化 300 多种蛋白质的磷酸化,这些蛋白质与调节多种细胞功能有关,例如信号转导、转录控制、细胞凋亡和细胞周期。

Casein Kinases (CKs), a group of ubiquitous Ser/Thr kinases, regulate a wide range of cellular functions in eukaryotes, including phosphorylation of proteins that are substrates for degradation via the ubiquitin-proteasome system (UPS). Two casein kinases, casein kinase-1 (CK-1) and casein kinase-2 (CK-2), have been characterized from many sources.

CK1 kinases exist in at least seven isoforms (α, β, γ1-3, δ, and ɛ) in mammals and CK1 kinases phosphorylate various substrates to play vital roles in diverse physiological processes such as DNA repair, cell cycle progression, cytokinesis, differentiation, and apoptosis. Casein kinase 2 (CK2) is a highly pleiotropic serine-threonine kinase, which catalyzed phosphorylation of more than 300 proteins that are implicated in regulation of many cellular functions, such as signal transduction, transcriptional control, apoptosis, and the cell cycle.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-169713
    CK1δ-IN-5 Inhibitor
    CK1δ-IN-5 (Compound 24) 是一种酪蛋白激酶 1δ (CK1δ) 抑制剂。CK1δ-IN-5 可用于神经退行性疾病的研究。
    CK1δ-IN-5
  • HY-172676
    GW461484A Inhibitor
    GW461484A 是一种靶向 Candida albicans Yck2 的小分子抑制剂,IC50 为 0.11 µM。GW461484A 对 C. albicansMIC80 为 12.5 µM。GW461484A 有望用于真菌性疾病研究,如耐药型念珠菌感染。
    GW461484A
  • HY-163783
    CSNK2-IN-1 Inhibitor
    CSNK2-IN-1 是一种强效的,具有选择性的 CSNK2 抑制剂,对 CSNK2A1CSNK2A2IC50 分别为 1.7 nM 和 0.66 nM。CSNK2-IN-1 对 β-冠状病毒 (如 SARS-CoV-2 和 MHV) 具有抗病毒活性。CSNK2-IN-1 具有良好的溶解度、代谢稳定性和低细胞毒性,但在体内血浆浓度迅速下降,不足以达到药理作用,可用于抗病毒药物开发的研究。
    CSNK2-IN-1
  • HY-163182
    CSNK2A-IN-2 Inhibitor
    CSNK2A-IN-2 (compound 6c) 是选择性的 CSNK2A 抑制剂,具有抗病毒活性。CSNK2A-IN-2 表现出对病毒复制的抑制作用,和对 PIM3 的选择性。
    CSNK2A-IN-2
  • HY-W840382
    CK1δ-IN-8 Inhibitor
    CK1δ-IN-8 (Compound 429) 是一种 CK1δ 抑制剂,可用于阿尔兹海默症领域研究。
    CK1δ-IN-8
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