Catalog No.: PC-35680Not For Human Use, Lab Use Only.
KCI807 (KCI-807) is a small molecule that selectively disrupts ELK1-dependent promoter activation by wild-type and variant androgen receptors (IC50=0.53 uM) without interfering with ELK1 activation by ERK.
KCI807 (KCI-807) is a small molecule that selectively disrupts ELK1-dependent promoter activation by wild-type and variant androgen receptors (IC50=0.53 uM) without interfering with ELK1 activation by ERK.
KCI807 binds to AR (Kd=69.2 nM), blocking ELK1 binding, and selectively blocks recruitment of AR to chromatin by ELK1.
KCI807 primarily affects a subset of AR target growth genes selectively suppressing AR-dependent growth of PC cell lines with a better inhibitory profile than Enzalutamide.
KCI807 also inhibits in vivo growth of castration/enzalutamide-resistant cell line-derived and patient-derived tumor xenografts.
Physicochemical Properties
M.Wt
254.241
Formula
C15H10O4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
5-hydroxy-2-(3-hydroxyphenyl)-4H-chromen-4-one
References
1. Rosati R, et al. Clin Cancer Res. 2018 Sep 5. pii: clincanres.0982.2018. doi: 10.1158/1078-0432.CCR-18-0982.
