For research use only. Not for therapeutic Use.
PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer[1].
PS121912 behaves like a VDR antagonist at low concentrations but interacts with more targets at higher concentrations leading to apoptosis mediated by caspase 3/7 activation[1].
PS121912 (combined with 1,25-(OH)2D3)reduces the transcription levels of cyclin A and D thus arresting HL-60 cells in the S or G2/M phase[1].
PS121912 shows an acceptable metabolic stability and can inhibit the metabolic enzyme CYP3A4 at higher concentrations in vivo cancer studies[1].
| Catalog Number | I035115 |
| CAS Number | 1529814-60-5 |
| Synonyms | N-[(4-methoxyphenyl)-(2-methyl-1H-indol-3-yl)methyl]-4-(trifluoromethyl)aniline |
| Molecular Formula | C24H21F3N2O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H21F3N2O/c1-15-22(20-5-3-4-6-21(20)28-15)23(16-7-13-19(30-2)14-8-16)29-18-11-9-17(10-12-18)24(25,26)27/h3-14,23,28-29H,1-2H3 |
| InChIKey | NNTQFFZNUZBJND-UHFFFAOYSA-N |
| SMILES | CC1=C(C2=CC=CC=C2N1)C(C3=CC=C(C=C3)OC)NC4=CC=C(C=C4)C(F)(F)F |
| Reference | [1]. Sidhu PS, et al. Anticancer activity of VDR-coregulator inhibitor PS121912. Cancer Chemother Pharmacol. 2014;74(4):787-798. |
