xpo1

Eltanexor (ONO-7706) is an orally active exportin-1 (XPO1) inhibitor. It has effective anti-leukemic activity. Eltanexor inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor causes caspase-dependent apoptosis in a panel of leukemic cell lines.

Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1 exportin 1 by covalent modification at a cysteine residue.

XPO1-ligand-1 is a target protein ligand for XPO1, and it can be utilized in the synthesis of PROTAC XPO1 degrader-1.

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.

XPO1-IN-1 is an orally active XPO1 inhibitor capable of acting on MM.1S cells (IC50: 24 nM). XPO1-IN-1 effectively induces cell cycle arrest and apoptosis. XPO1-IN-1 exhibits good metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used to study multiple myeloma.

Verdinexor (KPT-335) (KPT-335), a specific XPO1 CRM1 inhibitor, are orally bioavailable.

(E)-KPT330 is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.

SP100030 analogue 1 (compound 11) is a selective transcription activation (SITA) inhibitor within the SP100030 class, capable of inhibiting XPO1-dependent upregulation of IL2 in a Jurkat-based IL2-Luc reporter assay, with an EC50 of 137 nM.

CW0134 (Compound 12) serves as a modulator for exportin1 (XPO1), disrupting chromatin binding and inhibiting NFAT transcription factors and T cell activation [1].

E3 ligase Ligand 49 is an E3 ubiquitin ligase ligand. It is utilized in the synthesis of PROTACs.

KPT-251 is a selective nuclear export inhibitor.