| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 0.1 mg/mL (insoluble)
DMSO : 130 mg/mL (320.71 mM)
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| Keywords | Inhibitor | UT155 | inhibit | Androgen Receptor | UT-155 | UT 155 |
| Inhibitors Related | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2,2,5,7,8-Pentamethyl-6-Chromanol | S-23 | Bavdegalutamide | Enzalutamide | Adrenosterone | Allura Red AC | SK33 | Sunset Yellow FCF | Ostarine | Flutamide |
| Related Compound Libraries | Nuclear Receptor Compound Library | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Prostate Cancer Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Transcription Factor-Targeted Compound Library |
United States
