1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. CRM1

CRM1 (染色体维持蛋白1)

Chromosomal Maintenance 1; Exportin 1; XPO1

CRM1 (Chromosome region maintenance 1; Exportin 1; XPO1), a member of the karyopherin β family of transport receptors, is an important nuclear protein export receptor that recognizes hydrophobic, leucine-rich nuclear export signal (NES) and transports target proteins across a Ran-GTP gradient. CRM1 is involved in the active transport of a number of cargo proteins, including transcription factors, tumor suppressor proteins (TSPs), and cell-cycle regulators, such as p53, p21, p27, nucleophosmin 1 (NPM1), as well as RNA molecules.

Abnormal CRM1 upregulation can have several cancer-promoting consequences. Upregulation of CRM1 would allow more growth regulatory proteins, such as c-myc or BCR-ABL, to be transported into the cytoplasm and activate downstream signaling leading to sustained cell proliferation. Similarly, tumor suppressor proteins (TSPs), such as Rb, p53, p21, or p27, are functionally inactivated upon export, hence removing the check on inappropriate cell growth. Similar disruptions would occur in the processes of apoptosis, DNA damage repair, chromosomal stabilization, and angiogenesis, just to name a few examples. Hence, inhibition of CRM1 activity became an attractive therapeutic target.

CRM1 相关产品 (6):

目录号 产品名 作用方式 纯度
  • HY-16909
    Leptomycin B


    Inhibitor 99.54%
    Leptomycin B (CI 940; LMB) 是一种蛋白出核转运抑制剂。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1/exportin 1 失活。 Leptomycin B 是一种有效的抗真菌抗生素,可阻断真核细胞周期。
  • HY-100423A
    Eltanexor Z-isomer Inhibitor
    Eltanexor Z-isomer (KPT-8602 Z-isomer) 是活性较弱的KPT-8602异构体。KPT-8602为高效的CRM1抑制剂。
  • HY-146384
    CRM1 degrader 1
    CRM1 degrader 1 (1l) 是一种低毒的染色体区域维护 1 (CRM1) 降解剂。CRM1 是几种肿瘤抑制因子的唯一核输出蛋白,这是一种生长调节蛋白,是一种有吸引力的癌症药物靶点。CRM1 degrader 1 诱导胃癌凋亡 (Apoptosis) 并选择性抑制胃癌的增殖。
  • HY-114597
    PKF050-638 Inhibitor
    PKF050-638 是一种有效且具有选择性的 HIV-1 Rev 抑制剂 (IC50=0.04 μM)。 PKF050-638 通过破坏 CRM1-NES 相互作用抑制 CRM1 介导的 Rev 核输出。
  • HY-117996
    KPT-251 Inhibitor
    KPT-251 是一种具有口服活性的染色体区域维持1蛋白 (CRM1) 抑制剂。 KPT-251 诱导癌细胞凋亡 (apoptosis),具有抗白血病活性。
  • HY-N6795
    Leptomycin A


    Inhibitor ≥99.0%
    Leptomycin A 是链霉菌的代谢物,是 CRM1 的抑制剂,阻断CRM1和核出口信号相互作用,阻止多种蛋白质的核出口。Leptomycin A 抑制 HIV-1的复制。活性略低于 Leptomycin B。