生物活性 | |||
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描述 | Retinoid X receptors occupy a central position in the nuclear receptor superfamily for the heterodimers formed by RXRs with many other family members are involved in the control of a variety of (patho)physiologic processes. UVI 3003 is a potent and selective RXR antagonist, used as a tool to test the contribution of RXR to transactivation by a given RXR heterodimer. UVI 3003 at concentration of 10μM could almost completely reverse depression of proliferation and increased apoptosis by combined RAR and RXR agonists in PLB985 cells in 12 days, but did not significantly affect growth inhibition or apoptosis in NB4 cells exposed to RAR agonists possibly because of the obliteration of the RXR requirement for apoptosis due to PML-RAR fusion protein. UVI 3003 can fully antagonize CD3254, a potent RXR agonist, induced transcription through Gal4-RXR in HeLa cells stably transfected with the reporter recombinant 5xGal4-βGlo-Luc and Gal4-hRXRβ. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.45mL 2.29mL 1.15mL |
22.91mL 4.58mL 2.29mL |