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.

CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activity.CBS9106 inhibits CRM1-dependent nuclear export and reduces CRM1 protein levels.CBS9106 inhibits tumor growth and prolongs the survival of mice bearing tumor xenografts.CBS9106 is an inhibitor of CRM1-dependent nuclear export and reduces CRM1 protein levels.

KPT185 (KPT 185) is a selective CRM1 inhibitor, inducing apoptosis, cell-cycle arrest.

Leptomycin A, a metabolite derived from Streptomyces, acts as an inhibitor of CRM1 (exportin 1) and effectively suppresses HIV-1 replication. Compared to Leptomycin B, it exhibits lesser potency. Leptomycin A hampers the interaction between CRM1 and nuclear export signals, effectively hindering the nuclear export of a wide array of proteins.

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.

CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor of CRM1, localizing it to the nuclear periphery, reducing its nuclear presence, and inhibiting its nuclear export function. It effectively inhibits the growth of colorectal cancer cells and induces apoptosis [1].

CRM1-IN-1 (Compound KL1), a noncovalent inhibitor of CRM1, promotes nuclear degradation of CRM1 with an IC50 of 0.27 μM, inhibits CRM1-mediated nuclear export, suppresses cell proliferation, and induces apoptosis in colorectal cancer cells [1].