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。 来那度胺(191732-72-6)是一种萨利度胺类似物,与萨利度胺1一样,与小脑结合,小脑是一种culincin依赖性泛素连接酶的底物识别成分,并抑制其自二素化活性2。 诱导T细胞抑制因子Ikaros (IKZF1)和Aiolos (IKZF3)的降解导致T细胞激活 来那度胺对多发性骨髓瘤细胞IKZF1和IKZF3的选择性抑制可导致细胞死亡。 细胞渗透。 警告:产生畸形的 。
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
CAS:
191732-72-6
Catalog Number:
10-2148
Activity:
Immunomodulator
Chemical Name:
(R,S)-3-(4-Amino-1-oxo-3H-isoindol-2-yl)piperidine-2,6-dione
Molecular Weight:
259.26
Molecular Formula:
C13H13N3O3 Solubility:
Soluble in DMSO (up to 30 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
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