WWL0245,2869057-11-2

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WWL0245

CAS No. : 2869057-11-2

MCE 国际站：WWL0245

产品活性：WWL0245 是一种有效的选择性 BRD4 PROTAC。WWL0245 选择性降解 BRD4 的 DC₅₀ <1 nM, 降解 BRD2/3 和 PLK1 的 DC₅₀ >1 μM)。WWL0245 在 BETi 敏感的癌细胞系，包括 AR 阳性前列腺癌细胞系中表现出优异的选择性细胞毒性。WWL0245 是 AR 阳性前列腺癌研究中有前景的候选药物，也是研究 BRD4 生物学功能的有价值的工具化合物。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: WWL0245 (0-1 μM; 96h) suppresses the proliferation of AR-positive prostate cancer cells with IC₅₀ values range from 0.0159 μM -10 μM. It shows greater antiproliferative activity to AR-positive cell lines VCaP, LNCaP, 22Rv1 with IC₅₀ values of 0.016 μM, 0.021 μM, 0.053 μM, respectively.
WWL0245 (1 μM; 24 hours) results in the downregulation of BRD4 and c-Myc in a time-dependent manner in LNCaP, 22Rv1, VCaP cell lines and results in the decrease of BRD4 level and c-Myc level in a concentration-dependent manner in 22Rv1 and VCaP cell with DC50 of sub-nanomolar. But WWL0245 could also downregulate BRD4 level in DU145 cells but has negligible effects in c-Myc level.
WWL0245 (100 nM-1 μM; 24 hours) suppresses the transcription of AR-regulated genes (PSA, TMPRSS2, ERG, FKBP5, BMPR1B) at various degrees.

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