crm1

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.

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.

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.

(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.

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

KPT-251 is a selective nuclear export inhibitor.

KPT276 (KPT 276) is an orally bioavailable selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of CRM1.

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

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

CRM1 degrader 1 (1l) is a low-toxicity CRM1 degrader that induces apoptosis in gastric carcinoma and selectively inhibits the proliferation of gastric cancer[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].

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].

Eltanexor Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC50s of 100 nM-50 μM, < 100 nM, > 30 μM, respectively.Eltanexor Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.

PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction. PKF050-638 is an effective and selective inhibitor of HIV-1 Rev (IC50=0.04 μM).

Selinexor HCl (1393477-72-9 free base) is an oral selective XPO1 (XPO1/CRM1) inhibitor that induces cell cycle arrest and apoptosis in tumor cells by blocking the transport of tumor suppressor proteins from the nucleus to the cytoplasm, thereby promoting their accumulation within the nucleus. Selinexor has been studied for the treatment of malignant tumors such as multiple myeloma.

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.

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.

CW8001 is a covalent Exportin-1 (XPO1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. It prevents the nuclear localization of NFAT transcription factors, thereby suppressing the expression of inflammatory cytokines like IL-2. CW8001 shows potential for research in T cell-driven immune diseases such as graft-versus-host disease (GVHD).

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

CRM1-IN-3 (B28), a noncovalent inhibitor of CRM1, is utilized in the research of protein localization and tumor studies [1].

Diphtheria toxin CRM197 is a nontoxic variant of the diphtheria toxin, characterized by a single mutation [substitution of glycine with glutamic acid at position 52], which eliminates its toxicity. CRM197 is widely used as a carrier protein in vaccines.

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

CW2158 (Compound 13) is a modulator of exportin1 (XPO1). It disrupts chromatin binding and inhibits the activation of NFAT transcription factors and T cells.