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You are here:Home-Inhibitors & Agonists-Membrane Transporter/Ion Channel-Exportin-1 (CRM1,XPO1)

Request The Product List ofExportin-1 (CRM1,XPO1) Exportin-1 (CRM1,XPO1)

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.

Cat. No. Product Name CAS No. Information
H8740

Felezonexor

 		1076235-04-5

Felezonexor is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences; 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, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression.
H4367

Verdinexor

 		1392136-43-4

Verdinexor (KPT-335, KPT335) is an orally bioavailable, selective inhibitor of nuclear export (SINE), inhibits the function of nuclear export protein Exportin 1 (XPO1/CRM1) and the viability of Jurkat and canine DLBCL cells with IC50 of 8.7 nM and 13.3 nM, respectively; induces apoptosis in CLBL1 cells and primary canine DLBCL cells; reduces influenza a virus replication in vitro and in vivo; also inhibits XPO1-mediated transport and reduces RSV replication in vitro, shows effectivity against RSV A and B strains and reduces viral replication following prophylactic or therapeutic administration.
H4366

Selinexor

 		1393477-72-9

Selinexor (KPT-330, KPT330) is a potent, orally available, selective inhibitor of nuclear export (SINE) targeting CRM1 (XPO1); demonstrates in vivo anti-leukaemic efficacy against T-ALL and acute myeloid leukaemia (AML) cells; triggers nuclear accumulation of multiple CRM1 cargo tumor suppressor proteins followed by growth arrest and apoptosis in MM cells, block c-Myc, Mcl-1, and NF-κB activity. Selinexor (KPT-330, KPT330) induces proteasome-dependent CRM1 protein degradation, upregulates CRM1, p53-targeted, apoptosis-related, anti-inflammatory and stress-related gene transcripts in MM cells.
H4365

Leptomycin B

 		87081-35-4

A potent and specific nuclear export inhibitor that binds to and inhibits CRM1 (XPO1); blocks the cell cycle and shows potent anti-tumor activity, blocks the nuclear export of many proteins including HIV-1 Rev, MAPK/ERK, and NF-κB/IκB, and inhibits the inactivation of p53.
H4364

KPT-8602 Z-isomer

 		1642300-78-4

The Z-isomer of Eltanexor (KPT-8602), which is a second-generation SINE with markedly reduced brain penetration compared to selinexor.
H4363

KPT-251

 		1388841-50-6

A small-molecule, selective inhibitor of nuclear export (CRM1 inhibitor;SINE) that exhibits potent antileukemic activity; induces apoptosis at nanomolar concentrations in a panel of human AML cell lines with negligible toxicity to normal hematopoietic cells.
H4362

Eltanexor

 		1642300-52-4

A second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor with markedly reduced brain penetration compared to selinexor (30-fold less); inhibits viability of human AML cell lines in vitro with IC50 of 20−211 nM, more active than the first-generation XPO1 inhibitor, selinexor; exhibits greater anti-leukemic efficacy against both leukemic blasts and LICs in AML patient-derived xenograft models, with no effect on normal hematopoietic stem and progenitor cell (HSPC) frequency.

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