CRM1
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.
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CRM1 Related Products (30)
Related Products (30)
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Antibodies (1)
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Selinexor
0 ImagesSynonyms: KPT-330Selinexor (KPT-330) is an analog of KPT-185 (HY-15611). Selinexor is an orally active, selective CRM1 inhibitor that inhibits tumor growth by inducing PANoptosis.
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Leptomycin B
0 ImagesSynonyms: CI 940; LMBLeptomycin 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.
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Eltanexor
0 ImagesSynonyms: KPT-8602Eltanexor (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.
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Verdinexor
0 ImagesSynonyms: KPT-335Verdinexor (KPT-335) is an orally active inhibitor for selective inhibitor of nuclear export (SINE). Verdinexor inhibits the respiratory syncytial virus A2 (RSV A2) replication with an IC50 of 0.96 µM. Verdinexor inhibits the function of nuclear export protein Exportin 1 (XPO1/CRM1), inhibiting pro-inflammatory responses. Verdinexor exhibits antitumor effciency.
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KPT-276
0 ImagesKPT-276 is an orally active and blood-brain barrier-penetrant selective XPO1/CRM1 inhibitor. KPT-276 blocks XPO1-mediated nuclear export function and promotes nuclear retention of various tumor suppressor proteins. KPT-276 induces apoptosis and G1 cell cycle arrest in tumor cells, and downregulates c-MYC, CDC25A, and BRD4. KPT-276 reduces immune cell proliferation through nuclear accumulation of cell cycle inhibitors, rescues TDP-43 cytoplasmic mislocalization, and restores axon growth and growth rate in mutant PFN1 motor neurons. KPT-276 maintains axonal cytoskeletal integrity and mitochondrial function, and inhibits tumor growth. KPT-276 can be used for research on glioblastoma, non-Hodgkin lymphoma, amyotrophic lateral sclerosis, multiple myeloma, and non-small cell lung cancer.
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PROTAC XPO1 degrader-1
0 ImagesPROTAC XPO1 degrader-1 is a CRBN-recruiting PROTAC degrader of exportin 1 (XPO1), with a DC50 of 23.67 nM. It exerts anti-proliferative effects against acute myeloid leukemia cells by inducing XPO1 protein degradation, inhibiting NF-κB activity, inducing apoptosis, and causing G1 cell cycle arrest. PROTAC XPO1 degrader-1 can be used for research on acute myeloid leukemia.
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FR-027
0 ImagesFR-027 is an orally active, blood-brain barrier permeable XPO1 inhibitor with an EC50 value of 54-69 nM in human cells. FR-027 covalently modifies Cys528 of XPO1 via nucleophilic aromatic substitution, maintaining the nuclear export signal binding groove of XPO1 in a closed conformation to block the nuclear export process, and inhibits XPO1 function without inducing its protein degradation. FR-027 promotes cancer cell apoptosis and inhibits the growth of hematological and solid tumor cells. FR-027 can be used in research related to acute lymphoblastic leukemia, ovarian cancer, glioblastoma, and primary central nervous system lymphoma.
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Felezonexor
0 ImagesSynonyms: CBS9106; SL-801
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Eltanexor Z-isomer
0 ImagesCat. No.: HY-100423ACAS No.: 1642300-78-4Synonyms: KPT-8602 (Z-isomer)Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.
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Leptomycin A
0 ImagesCat. No.: HY-N6795CAS No.: 87081-36-5
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Selinexor (Standard)
0 ImagesSynonyms: KPT-330 (Standard)Selinexor (Standard) is the analytical standard of Selinexor. This product is intended for research and analytical applications. Selinexor (KPT-330) is an analog of KPT-185 (HY-15611). Selinexor is an orally active, selective CRM1 inhibitor that inhibits tumor growth by inducing PANoptosis.
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CW8001
0 ImagesCat. No.: HY-174132CW8001 is a covalent XPO1 (Exportin-1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. CW8001 prevents nuclear localization of NFAT transcription factors, suppressing expression of inflammatory cytokines like IL-2. CW8001 is promising for research of T cell-driven immune diseases such as graft-versus-host disease (GVHD).
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CRM1-IN-2
0 ImagesCat. No.: HY-155972ACAS No.: 3032506-81-0CRM1-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.
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CW2158
0 ImagesCat. No.: HY-161392CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells.
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CRM1-IN-1
0 ImagesCat. No.: HY-155972CAS No.: 3032506-80-9CRM1-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.
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