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

CRM1

Chromosome maintenance protein 1 (CRM1) is a nuclear export receptor involved in the active transport of tumor suppressors (eg, p53 and nucleophosmin) whose function is altered in cancer because of increased expression and overactive transport. Blocking CRM1-mediated nuclear export of such proteins is a novel therapeutic strategy to restore tumor suppressor function. Orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein have been recently developed.

CRM1 is the sole exporter of many tumor-suppressor proteins (TSPs), and functions as a proto-oncogene by transporting these tumor suppressors from the nucleus, where they are active, to the cytoplasm, where their activity is abrogated.

CRM1 相关产品 (9):

Cat. No. Product Name Effect Purity
  • HY-17536
    Selinexor Inhibitor 99.82%
    Selinexor (KPT-330),是 KPT-185 的类似物,是一种口服活性的,CRM1 的选择性抑制剂。
  • HY-16909
    Leptomycin B Inhibitor 99.84%
    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-100423
    Eltanexor Inhibitor 99.71%
    Eltanexor (KPT-8602) 是第二代高特异性的,具有口服活性的 exportin-1 (XPO1) 抑制剂,具有较强的抗白血病活性。Eltanexor (KPT-8602) 通过直接靶向 XPO1 抑制 XPO1 依赖的核输出 (EC50=60.9 nM)。Eltanexor (KPT-8602) 诱导白血病细胞株 caspase 依赖性凋亡。
  • HY-17539
    KPT-276 99.05%
    KPT-276 是KPT-185的类似物,是一种口服生物可利用的核输出选择性抑制剂(SINE),它不可逆地与CRM1结合并阻断CRM1的功能。
  • HY-15970
    Verdinexor Inhibitor 99.97%
    Verdinexor(KPT-335)是新型口服活性出核抑制剂(SINE),能有效抑制犬肿瘤细胞系出核蛋白Exportin 1(XPO1/CRM1),也能降低流感病毒的复制水平。
  • HY-N6795
    Leptomycin A Inhibitor
    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。
  • 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-15611
    KPT-185 98.24%
    KPT-185 是一种口服生物可利用的 CRM1 选择性抑制剂,在亚微摩尔浓度下显示出有效的抗增殖特性 (IC50=100-500 nM),诱导 AML 细胞系和患者母细胞凋亡、细胞周期停滞和髓样分化。
  • HY-108716
    CBS9106 Inhibitor
    CBS9106 (SL-801) 是一种可逆的口服 CRM1 抑制剂,具有 CRM1 降解和抗肿瘤活性。CBS9106 抑制 CRM1 依赖性核出口,以时间和剂量依赖的方式使癌细胞周期停滞并诱导其凋亡。
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