STF-083010 is a novel Ire1 inhibitor which can Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. STF-083010 at 60μM inhibited endogenous XBP1 mRNA splicing in RPMI 8226 cells treated with 300nM thapsigargin. It inhibited the production of sXBP1 protein, but not the autophosphorylation of Ire1α, at 60μM in MM1.S and RPMI 8226 cell lines treated with 300nM thapsigargin. STF-083010 at 60mg/kg blocked bortezomib (1mg/kg)-induced XBP1 activity in vivo. Administration of STF-083010 at 30mg/kg, i.p., once weekly for 2 weeks, decreased tumor growth of NOD/SCID/IL2Rγ null mice xenograft RPMI 8226 tumor. STF-083010 was preferentially toxic to freshly isolated human CD138+ MM cells compared with other similarly isolated cell populations[2].
STF-083010 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
SF21 cell
Function assay
Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=9.939 μM
Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=9.939 μM
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