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.

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.

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

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.