Nuclear Translocation Regulators

The cell nucleus controls the entry and exit (translocation) of its larger molecules from/to the cytoplasm. Small molecules can enter the nucleus easily, but macromolecules such as RNA and proteins enter the nucleus only when assisted by substances called importins. For large molecules to leave the nucleus, exportins are required. Importin proteins bind with molecules in the cytoplasm, after which they are able to interact with the nuclear pore complex and pass through its channel into the nucleus. For large molecules leaving the nucleus, exportin binds with the molecule and diffuses to the cytoplasm of the cell. Nuclear translocation regulators affect the actions of importin and exportin and can be manipulated in order to affect the translocation of molecules.

The ability to control the movement of substances from and to the cytoplasm is of great use in research involving large molecule translocation. Sigma-Aldrich has a variety of products to aid research on the mechanisms and effects of nuclear translocation.

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SRP3258 DKK-1 human recombinant, expressed in HEK 293 cells, ≥97% (SDS-PAGE), ≥97% (HPLC), cell culture tested DKK-1 (dickkopf WNT signaling pathway inhibitor 1) was originally identified as a Xenopus head forming molecule that behaves as an antagonist for Wnt signaling. Subsequent studies have shown that DKK-1 play an important regulatory role in the Wnt/β-catenin signaling pathway by forming inhibitory complexes with LDL receptor-related proteins 5 and 6 (LRP5 and LRP6), which are essential components of the Wnt/β-catenin signaling system. It has been suggested that by inhibiting Wnt/β-catenin signaling, which is essential for posterior patterning in vertebrates, DKK-1 permits anterior development. This notion is supported by the finding that mice deficient of DKK-1 expression lack head formation and die during embryogenesis. In bladder cancer, DKK-1 is overexpressed in serum and might be associated with tumor progression. It is also associated with multiple myeloma and affects bone formation. Changes in serum levels of DKK1 is linked with inflammation in rheumatoid arthritis. In the process of development, tumorigenesis, and inflammation, DKK1 enhances angiogenesis.
SML1390 Fexaramine ≥98% (HPLC) Fexaramine is a potent and selective agonist of the bile acid sensor farnesoid X receptor (FXR) in the gut with an EC50 of 25 nM and no activity found for other nuclear receptors. Fexaramine induces enteric fibroblast growth factor 15 (FGF15), causing alterations in bile acid composition without activating FXR target genes in the liver. In mouse studies, fexaramine enhanced thermogenesis and browning of white adipose tissue while reducing diet-induced weight gain, body-wide inflammation and hepatic glucose production. Fexaramine also improved insulin responsiveness.
Fexaramine might regulate lipid and glucose metabolism and can serve as a therapeutic target in the treatment of fatty liver disease, type 2 diabetes and obesity. Fexaramine might mediate cholesterol homeostasis and promotes osteoblast differentiation and suppresses differentiation of osteoclast.
G5172 GW4064 ≥97% (HPLC) GW4064 is a FXR agonist. GW4064 is a potent (EC50 = 15 nM), non-steroidal agonist of the orphan nuclear receptor FXR. It shows no activity on other nuclear receptors including RAR up to 1 mM. This is an important tool for the study of the involvment of FXR in a variety of biological activities.
SML1911 INI-43 ≥98% (HPLC) INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as that of its cargo transcription factors, NFY, AP-1, p65, and NFAT. INI-43 exhibit specific cytotoxicity toward cancer cells. INI-43 inhibits tumor growth in cancer xenograft models.
INI-43 is also known as (3-(1H-benzimidazol-2-yl)-1-(3-dimethylaminopropyl)pyrrolo[5,4-b]quinoxalin-2-amine). It has the ability to prevent the development of dermatologically xenografted esophageal and cervical tumor cells. INI-43 can also decrease activator protein 1 (AP-1) transcriptional activity, induced by phorbol-12-myristate-13-acetate (PMA).
L2913 Leptomycin B solution from Streptomyces sp. ≥95% (HPLC), Supplied in methanol: water (7:3) Leptomycin B is an unsaturated, branched-chain fatty acid, and is an important tool in the study of nuclear export. Leptomycin B is a specific inhibitor of proteins containing nuclear export signal. Leptomycin B inhibits nucleo-cytoplasmic translocation of molecules such as the HIV-1 Rev protein and Rev-dependent export of mRNA. The addition of very small amounts to fibroblasts causes accumulation of MEK in the nucleus. Other proteins that are influenced by leptomycin B are actin, c-Abl, cyclin B1, MDM2/p53, IκB, MPF, and PKA. The suggested inhibition mechanism involves the direct binding of leptomycin B to CRM1, which blocks the binding of CRM1 to proteins containing the nuclear export signal, via the interaction with cysteine residue in CRM1 control conserved region.
SML1604 NDB ≥98% (HPLC) NDB is a selective antagonist of human Farnesoid X receptor α (FXRα) that effectively modulates FXRα down-stream genes.
PZ0267 WAY-362450 ≥98% (HPLC) WAY-362450 is a potent and selective Farnesoid X receptor (FXR) agonist that lowers total plasma cholesterol (all lipoprotein species). WAY-362450 reduced the levels of high-density lipoprotein cholesterol (HDLc) in Cynomolgus monkeys, mice and hamsters. Apparently HDL lowering is achieved through increased transhepatic cholesterol efflux.
X4753 XCT790 ≥98% (HPLC), solid XCT790 is a potent and specific inverse agonist of ERRα. XCT790 is selective; showing no significant antagonist activity on related nuclear receptors, such as ERRγ or ERα at concentrations below 10 μM. XCT790 inhibits the constitutive activity of ERRα in both biochemical and cell-based assays. The IC50 value is 300-500 nM in transient transfection assays using GAL4-ERR LBD or full-length ERR with the mSHP promoter.