An essential nuclear protein export receptor known as CRM1 (Chromosome Region Maintenance 1; Exportin 1; XPO1), which belongs to the karyopherin family of transport receptors, recognizes hydrophobic, leucine-rich nuclear export signals (NES) and transports target proteins across a Ran-GTP gradient. Numerous cargo proteins, including transcription factors, tumor suppressor proteins (TSPs), cell-cycle regulators like p53, p21, p27, nucleophosmin 1 (NPM1), and RNA molecules are actively transported by CRM1.
Multiple consequences that can cause cancer can result from abnormal CRM1 upregulation. More growth regulatory proteins, like c-myc or BCR-ABL, could be transported into the cytoplasm and activate downstream signaling, resulting in sustained cell proliferation, if CRM1 were to be upregulated. Similar to Rb, p53, p21, or p27, tumor suppressor proteins (TSPs) are functionally inactivated upon export, removing the brake on uncontrollable cell growth. Apoptosis, DNA damage repair, chromosomal stabilization, and angiogenesis are just a few examples of processes that would be affected in a similar way. As a result, the therapeutic target of CRM1 activity inhibition became appealing.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V94852 | AN-988 | 340304-55-4 | AN-988 (Compound 6) is a covalent CRM1 inhibitor. |
|
V78397 | CRM1-IN-1 | CRM1-IN-1 (Compound KL1) is a non-covalent CRM1 inhibitor. | |
|
V78399 | CRM1-IN-2 | CRM1-IN-2 (Compound KL2) is a non-covalent CRM1 inhibitor. | |
|
V85410 | CRM1-IN-3 | 1114628-25-9 | |
|
V87146 | CW0134 | 1076235-18-1 | CW0134 (Compound 12) is a regulator of exportin1 (XPO1). |
|
V87145 | CW2158 | CW2158 (Compound 13) is a regulator of exportin1 (XPO1). | |
|
V20471 | Eltanexor (KPT-8602) | 1642300-52-4 | Eltanexor (is discontinued) formerly known as KPT-8602, is a second-generation exportin-1 inhibitor. |
|
V1589 | Selinexor (KPT-330) | 1393477-72-9 | Selinexor (also known as KPT-330) is an orally bioavailable, potent and selective CRM1 inhibitor. |
|
V98020 | SP100030 analogue 1 | 154934-68-6 | SP100030 analog 1 (Compound 11) is an analog of SP100030, a selective transcriptional activator (SITA) inhibitor, which inhibits XPO1-dependent IL2 upregulation in a Jurkat-based IL2-Luc reporter assay with an EC50 of 137 nM. |
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