Exportin-1
CRM1 is present in all eukaryotic cells, also known as exportin 1 or XPO1. It is responsible for the transport of over 200 proteins, which include many tumor suppressor proteins (TSP) and oncoproteins. CRM1 plays an essential role in mitosis through (I) binding and targeting key mitotic proteins to specific areas of the mitotic spindle; and (II) stabilizing the microtubule kinetochore to promote proper chromosomal segregation. Inhibition of RCC1, which regulates CRM1, by actinomycin D resulted in severe spindle assembly defects and mitotic catastrophe. Among the list of CRM1-mediated proteins are p53, FOXOs, p27, nucleophosmin, BCR-ABL, p21, PI3K/AKT, Wnt/β-catenin, NF-kB, APC, and Rb, all of which are significant targets in oncogenesis. Dysregulation of this transport process has been implicated in cancer, in addition to wound healing, inflammation, and viral infections. CRM1 overexpression has been demonstrated in both solid tumors and hematologic malignancies, and this overexpression is associated with a poorer prognosis and drug resistance.
References
1.Wang AY,et al. Stem Cell Investig. 2019;6:6. Published 2019 Feb 25.
References
1.Wang AY,et al. Stem Cell Investig. 2019;6:6. Published 2019 Feb 25.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
Exportin-1
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KPT-8602 Z-isomer
catalog no : M12493
cas no: 1642300-78-4
The Z-isomer of Eltanexor (KPT-8602), which is a second-generation SINE with markedly reduced brain penetration compared to selinexor. -
Eltanexor
catalog no : M12492
cas no: 1642300-52-4
A second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor. -
Selinexor
catalog no : M11640
cas no: 1393477-72-9
Selinexor (KPT-330, KPT330) is a potent, orally available, selective inhibitor of nuclear export (SINE) targeting CRM1 (XPO1). -
Verdinexor
catalog no : M11627
cas no: 1392136-43-4
Verdinexor (KPT-335, KPT335) is an orally bioavailable, selective inhibitor of nuclear export (SINE), inhibits the function of nuclear export protein Exportin 1 (XPO1/CRM1) and the viability of Jurkat and canine DLBCL cells with IC50 of 8.7 nM and 13.3 nM, respectively. -
KPT-251
catalog no : M11613
cas no: 1388841-50-6
A small-molecule, selective inhibitor of nuclear export (CRM1 inhibitor;SINE) that exhibits potent antileukemic activity.