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(+)-JJ-450 是一种非竞争性拮抗剂,专门针对雄激素受体 (AR),在不含雄激素的环境下能够抑制 AR 的核定位和转录活性。在 LN95 细胞中,(+)-JJ-450 抑制前列腺特异性抗原 (PSA) 表达的效果低于 (-)-JJ-450,可能是因为其靶向 AR 的配体结合域 (LBD)。通过促进未结合配体的 AR 在细胞核内降解并减少 AR 与雄激素反应元件 (AREs) 的结合,(+)-JJ-450 抑制 AR 及其剪切变体(如 ARv7)的转录活性。它能够用于 Enzalutamide (MDV3100) 耐药的去势抵抗性前列腺癌 (CRPC) 研究。

(+)-JJ-450 是一种非竞争性拮抗剂,专门针对雄激素受体 (AR),在不含雄激素的环境下能够抑制 AR 的核定位和转录活性。在 LN95 细胞中,(+)-JJ-450 抑制前列腺特异性抗原 (PSA) 表达的效果低于 (-)-JJ-450,可能是因为其靶向 AR 的配体结合域 (LBD)。通过促进未结合配体的 AR 在细胞核内降解并减少 AR 与雄激素反应元件 (AREs) 的结合,(+)-JJ-450 抑制 AR 及其剪切变体(如 ARv7)的转录活性。它能够用于 Enzalutamide (MDV3100) 耐药的去势抵抗性前列腺癌 (CRPC) 研究。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mg | 待询 | 10-14周 | |
| 50 mg | 待询 | 10-14周 |
(+)-JJ-450 相关产品
| 产品描述 | (+)-JJ-450 is a non-competitive antagonist that targets the androgen receptor (AR), inhibiting nuclear localization and transcriptional activity of AR under androgen-deprived conditions. In LN95 cells, (+)-JJ-450 is less effective than (-)-JJ-450 at inhibiting prostate-specific antigen (PSA) expression, likely due to its targeting of the AR ligand-binding domain (LBD). The compound works by promoting degradation of unbound AR within the nucleus and reducing AR binding to androgen response elements (AREs), thus inhibiting the transcriptional activity of AR and its splicing variants like ARv7. Additionally, (+)-JJ-450 is applicable for research in castration-resistant prostate cancer (CRPC) that is resistant to Enzalutamide (MDV3100). |
| 分子量 | 372.86 |
| 分子式 | C21H22ClFN2O |
| CAS No. | 1998094-24-8 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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