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

CRM1

Chromosomal Maintenance 1; Exportin 1; XPO1

CRM1

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17536
    Selinexor
    		Inhibitor 99.85%
    Selinexor (KPT-330), analog of KPT-185, is an orally bioavailable and selective CRM1 inhibitor.
    Selinexor
  • HY-16909
    Leptomycin B
    		Inhibitor 99.54%
    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
    Leptomycin B
  • HY-100423
    Eltanexor
    		Inhibitor 99.84%
    Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines.
    Eltanexor
  • HY-15970
    Verdinexor
    		Inhibitor 99.91%
    Verdinexor(KPT-335) is a novel, orally bioavailable selective inhibitor of nuclear export (SINE), inhibits nuclear export protein Exportin 1(XPO1/CRM1) against canine tumor cell lines; also reduce influenza virus replication in vitro and in vivo.
    Verdinexor
  • HY-15611
    KPT-185
    		98.21%
    KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts.
    KPT-185
  • HY-108716
    Felezonexor
    		Inhibitor 98.84%
    CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells.
    Felezonexor
  • HY-117996
    KPT-251
    		Inhibitor 99.92%
    KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity.
    KPT-251
  • HY-17539
    KPT-276
    		99.75%
    PKT-276, an analogue of PKT-185, is an oral bioavailable and selective inhibitor of nuclear output (SINE). PKT-276 is also a CRM1 antagonist that irreversibly binds to and blocks the function of CRM1.
    KPT-276
  • HY-100423A
    Eltanexor Z-isomer
    		Inhibitor
    Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.
    Eltanexor Z-isomer
  • HY-155972A
    CRM1-IN-2
    		Inhibitor
    CRM1-IN-2 (Compound KL2) is a noncovalent CRM1 inhibitor. CRM1-IN-2 localizes CRM1 in the nuclear periphery, depletes nuclear CRM1, and inhibits CRM1-mediated nuclear export. CRM1-IN-2 inhibits growth of colorectal cancer cells, and induces apoptosis.
    CRM1-IN-2
  • HY-161392
    CW2158
    		Modulator
    CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells.
    CW2158
  • HY-155972
    CRM1-IN-1
    		Inhibitor
    CRM1-IN-1 (Compound KL1) is a noncovalent CRM1 inhibitor. CRM1-IN-1 induces nuclear CRM1 degradation (IC50: 0.27 μM). CRM1-IN-1 inhibits CRM1-mediated nuclear export and cell proliferation, and triggers apoptosis in colorectal cancer cells.
    CRM1-IN-1
  • HY-161391
    CW0134
    		Modulator
    CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells.
    CW0134
  • HY-157412
    CRM1-IN-3
    		Inhibitor
    CRM1-IN-3 (B28) is a noncovalent CRM1 inhibitor. CRM1-IN-3 can be used for the research of protein localization and tumor.
    CRM1-IN-3
  • HY-114597
    PKF050-638
    		Inhibitor
    PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction.
    PKF050-638
  • HY-N6795
    Leptomycin A
    		Inhibitor ≥99.0%
    Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
    Leptomycin A
  • HY-146384
    CRM1 degrader 1
    CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer.
    CRM1 degrader 1
  • HY-157136
    LFS-1107
    LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research.
    LFS-1107
  • HY-17536R
    Selinexor (Standard)
    		Inhibitor
    Selinexor (Standard) is the analytical standard of Selinexor. This product is intended for research and analytical applications. Selinexor (KPT-330), analog of KPT-185, is an orally bioavailable and selective CRM1 inhibitor.
    Selinexor (Standard)
  • HY-163902
    SP100030 analogue 1
    		Inhibitor
    SP100030 analogue 1 (compound 11), a SP100030 (HY-110177) analogue, is a selective inhibitor of transcriptional activation (SITA) with an EC50 of 137 nM for suppressing the XPO1-dependent upregulation of IL2 by Jurkat-based IL2-Luc reporter assay.
    SP100030 analogue 1
Cat. No. Product Name / Synonyms Application Reactivity