Product Description: ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro[1].
Applications: Cancer-programmed cell death
Formula: C20H17N3O3S2
References: [1]Wu M, et al. Selective androgen receptor degrader (SARD) to overcome antiandrogen resistance in castration-resistant prostate cancer[J]. Elife, 2023, 12: e70700.
CAS Number: 920915-26-0
Molecular Weight: 411.50
Research Area: Cancer
Target: Androgen Receptor;Apoptosis
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