JJ-450 is a non-competitive antagonist of the androgen receptor (AR) that effectively inhibits both wild-type AR and the mutant variant ARF876L. With an IC50 ranging from 1-10 μM in PC3 cells, JJ-450 selectively binds to AR without competing with androgens for the ligand binding domain. It disrupts AR nuclear translocation and promotes the degradation of unliganded AR, leading to decreased transcriptional activity. This compound is relevant for research applications involving castration-resistant prostate cancer (CRPC), particularly in studies focusing on resistance to Enzalutamide.
JJ-450 is a non-competitive antagonist of the androgen receptor (AR) that effectively inhibits both wild-type AR and the mutant variant ARF876L. With an IC50 ranging from 1-10 μM in PC3 cells, JJ-450 selectively binds to AR without competing with androgens for the ligand binding domain. It disrupts AR nuclear translocation and promotes the degradation of unliganded AR, leading to decreased transcriptional activity. This compound is relevant for research applications involving castration-resistant prostate cancer (CRPC), particularly in studies focusing on resistance to Enzalutamide.
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