| Name | UT-155 |
| Description | UT-155 is a selective and potent antagonist of the androgen receptor (AR) with a binding affinity (Ki) of 267 nM for the AR ligand-binding domain (AR-LBD). |
| In vitro | UT-155 binds to the AR-LBD (Ki: 267 nM) and potently inhibits R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide's efficacy is halved against the W742L mutant AR. In LNCaP cells, UT-155 inhibits PSA and FKBP5 gene expression induced by 0.1 nM R1881 at concentrations between 10 and 100 nM, demonstrating 5-10 times better efficacy than enzalutamide. |
| In vivo | Consistent with its anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenografts by 53%, while enzalutamide has no effect. In UT-155-treated animals, tumor weights, PSA levels, and expression of AR and AR-SV are significantly reduced. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 0.1 mg/mL (insoluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (9.87 mM), Sonication is recommended.
DMSO : 130 mg/mL (320.71 mM), Sonication is recommended.
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| Keywords | UT-155 | UT155 | UT 155 | Inhibitor | inhibit | AR-LBD | AndrogenReceptor | androgen receptor |
| Inhibitors Related | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2-Ethylhexyl trans-4-methoxycinnamate | S-23 | Enzalutamide | Octinoxate | Testosterone propionate | Allura Red AC | Sunset Yellow FCF | Ostarine | 2-sec-Butylphenol | Flutamide |
| Related Compound Libraries | Nuclear Receptor Compound Library | Bioactive Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | NO PAINS Compound Library | Anti-Prostate Cancer Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Covalent Inhibitor Library | Anti-Cancer Compound Library | Transcription Factor-Targeted Compound Library |
United States
