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Nuclear Translocation Regulators

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Description	Biochem/physiol Actions	Product #
GW4716 ≥98% (HPLC), solid	GW4716 is an estrogen-related receptor γ (ERRγ) agonist. The ERRs generally are considered to be constitutively active receptors that interact with coactivator proteins in the absence of exogenous ligands. IC₅₀ value of 300-500 nM in transient transfection assays.	G5920
Leptomycin B from Streptomyces sp. 5 μg/mL in methanol: water (7:3), ≥95% (HPLC)	Leptomycin B is an unsaturated, branched-chain fatty acid, and is an important tool in the study of nuclear export. It is a specific inhibitor of proteins containing nuclear export signal. It 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.	L2913
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.	X4753

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