| S7252 |
Selinexor (KPT-330)
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Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. This compound is in Phase 2.
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Cell, 2025, S0092-8674(25)01149-3
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Sci Transl Med, 2025, 17(792):eadt5553
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J Clin Invest, 2025, 135(16)e187663
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| S7580 |
Leptomycin B (LMB)
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Leptomycin B (LMB, CI 940, Elactocin, Mantuamycin, NSC 364372) is a potent antifungal antibiotic isolated from Streptomyces and acts as a specific inhibitor of the nuclear export factor CRM1. Leptomycin B rapidly induces cytotoxic effects in cancer cell lines via covalent inhibition of CRM1 with IC50 values of 0.1 nM–10 nM.
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J Biol Chem, 2025, 301(9):110511
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Cells, 2024, 13(22)1855
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Biochem Biophys Rep, 2024, 39:101793
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| S8397 |
Eltanexor (KPT-8602)
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Eltanexor (KPT-8602, ONO-7706, ATG-016) is a second-generation, orally bioavailable XPO1 (also known as CRM1) inhibitor with IC50 values of 20–211 nM in 10 AML lines after 3 days exposure.
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Cell, 2025, S0092-8674(25)01149-3
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Blood Cancer Discov, 2025, 10.1158/2643-3230.BCD-25-0112
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J Transl Med, 2025, 23(1):62
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| S7125 |
KPT-185
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KPT-185 is a selective CRM1 inhibitor that induces growth inhibition and apoptosis in a panel of NHL cell lines with a median IC50 ~25 nM.
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PLoS One, 2025, 20(9):e0333127
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Cell Chem Biol, 2022, S2451-9456(22)00275-6
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Oncotarget, 2020, 11(36):3371-3386
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| S7707 |
Verdinexor (KPT-335)
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Verdinexor (KPT-335, ATG-527) is an orally bioavailable, selective XPO1/CRM1 inhibitor.
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J Transl Med, 2025, 23(1):62
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PLoS One, 2025, 20(9):e0333127
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J Biomed Sci, 2022, 29(1):44
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| S7251 |
KPT-276
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KPT-276 is an orally bioavailable selective CRM1 inhibitor.
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PLoS One, 2025, 20(9):e0333127
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Elife, 2021, 10e67587
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Front Oncol, 2020, 10:1424
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| S7551 |
Piperlongumine
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Piperlongumine (PPLGM, Piplartine), a natural alkaloid from Piper longum L., increases the level of reactive oxygen species (ROS) and selectively kills cancer cells. It is a direct TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1; also an inhibitor of PI3K/Akt/mTOR in human breast cancer cells.
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Biochim Biophys Acta Mol Basis Dis, 2025, 1871(3):167687
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Eur J Pharmacol, 2025, 997:177478
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PLoS One, 2025, 20(9):e0333127
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