1. Signaling Pathways
  2. PI3K/Akt/mTOR
  3. PIN1

PIN1 (肽基脯氨酰异构酶)

peptidylprolyl cis/trans isomerase, NIMA-interacting 1

PIN1 是一种肽酰脯氨酰异构酶(PPIase),能特异性识别 pSer/Thr-Pro 基序,催化脯氨酰酰胺键的顺式和反式异构化,改变底物蛋白的构象,从而影响其功能、稳定性或细胞内定位。PIN1 调控细胞周期蛋白如细胞周期蛋白 D (cyclin D)、细胞周期蛋白 E (cyclin E)、CDC25 等,从而调控 G1-S 过程和有丝分裂进程;PIN1 调控 p53、p73 等蛋白的稳定性,响应 DNA 损伤等应激信号,从而影响细胞周期停滞或凋亡;PIN1 调控 tau 蛋白的磷酸化,介导神经功能;PIN1 调控 NF-κB、JUN 等转录因子,介导免疫反应。 PIN1 功能障碍可能导致阿尔茨海默病、癌症、哮喘或微生物感染[1][2]

PIN1 is a peptidyl-prolyl isomerase (PPIase) that specifically recognizes the pSer/Thr-Pro motif, catalyzes the cis and trans isomerization of the proline amide bond, changes the conformation of the substrate protein, thereby affecting its function, stability or intracellular localization. PIN1 regulates cell cycle proteins such as cyclin D, cyclin E, and CDC25, thereby regulating the G1-S process and mitotic progression. PIN1 regulates the stability of proteins such as p53 and p73, responds to stress signals such as DNA damage, and thus affects cell cycle arrest or apoptosis. PIN1 regulates the phosphorylation of tau protein, mediating the neurological functions. PIN1 regulates transcription factors such as NF-κB and JUN, mediates immune responses. PIN1 dysfunction could lead to Alzheimer's disease, cancer, asthma, or microbial infection[1][2].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12135
    Poloxipan Inhibitor
    Poloxipan 是一种泛特异性 polo 样激酶 (PLK) 抑制剂,可以抑制激酶中称为 Polo-box 结构域 (PBD) 的 C 端非催化结构域。Poloxipan 对 PLK-1/2/3 的 PBD 的 IC50 分别为 3.2 μM、1.7 μM 和 3.0 μM。Poloxipan 同时还抑制其他磷酰氨基酸/磷酪氨酸结合域,如 CHK-2 的叉头关联 (FHA) 域、肽基脯氨酸顺/反异构酶 (PIN1) 的 WW 域和磷酪氨酸结合域 (STAT1/3/5 和淋巴细胞特异性蛋白酪氨酸激酶的 SH2 域)。Poloxipan 可用于肿瘤的研究。
    Poloxipan
  • HY-129310
    PIN1 inhibitor 5 Inhibitor
    PIN1 inhibitor 5 (compound 7) 是一种 PIN1 抑制剂 (Ki=0.08 μM),可用于癌症领域研究。
    PIN1 inhibitor 5
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