CRM1 Inhibitor

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.

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.

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.

Verdinexor (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.

KPT-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.

FR-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.

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.

KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity.

Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.

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.

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.

CW8001 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).

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-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.

AN-988 (compund 6) is a covalent CRM1 inhibitor.

CRM1-IN-3 (B28) is a noncovalent CRM1 inhibitor. CRM1-IN-3 can be used for the research of protein localization and tumor.

(2-(β-Piperidinoethyl)-9-hydroxyellipticinium chloride (compound 1AA) is a SETBP1 inhibitor that disrupts the interaction between SETBP1 and XPO1. (2-(β-Piperidinoethyl)-9-hydroxyellipticinium chloride inhibits colony formation, induces differentiation/cytotoxicity, and downregulates the transcription of Setbpl target genes. (2-(β-Piperidinoethyl)-9-hydroxyellipticinium chloride improves survival and reduces the spleen size of leukemic mice. (2-(β-Piperidinoethyl)-9-hydroxyellipticinium chloride can be used for myeloid neoplasms and solid tumors research.

Leptomycin B (Standard) is the analytical standard of Leptomycin B (HY-16909). This product is intended for research and analytical applications. 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 blocK_ing the eukaryotic cell cycle.

Selinexor-d₅ (KPT-330-d₅) isthe deuterium labeled Selinexor (HY-17536). Selinexor (KPT-330), an analog of KPT-185, is an orally active and selective CRM1 inhibitor.

Eltanexor Z-isomer (Standard) is the analytical standard of Eltanexor Z-isomer (HY-100423A). This product is intended for research and analytical applications. 0