Lenalidomide191732-72-6上海惠诚生物

Lenalidomide (191732-72-6) is a thalidomide analog which, like thalidomide1, binds to cereblon which is the substrate recognition component of a cullin-dependent ubiquitin ligase and inhibits its autoubiquitination activity2.  Induces degradation of T-cell repressors Ikaros (IKZF1) and Aiolos (IKZF3) leading to T cell activation.2  Selective inhibition of IKZF1 and IKZF3 by lenalidomide in multiple myeloma cells results in cell death.3,4 Cell permeable. Caution: Teratogenic   

References/Citations

1) Ito et al. (2010), Identification of a primary target of thalidomide teratogenicity; Science, 327 1345
2) Gandhi et al. (2014), Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T-cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4(CRBN); Br.J. Haematol., 164 811
3) Kronke et al. (2014), Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells; Science, 343 301
4) Lu et al. (2014), The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins; Science., 343 305