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Chemical Structure : AU-15330
CAS No.: 2380274-50-8
Catalog No.: PC-72798Not For Human Use, Lab Use Only.
AU-15330 (AU15330) is a highly specific and VHL-dependent PROTAC degrader of SWI/SNF ATPase components (SMARCA2, SMARCA4 and PBRM1), shows preferential cytotoxicity in enhancer-binding transcription factor-addicted cancers at low nanomolar concentrations.
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| 5 mg | $388 | In stock | |
| 10 mg | $598 | In stock | |
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AU-15330 (AU15330) is a highly specific and VHL-dependent PROTAC degrader of SWI/SNF ATPase components (SMARCA2, SMARCA4 and PBRM1), shows preferential cytotoxicity in enhancer-binding transcription factor-addicted cancers at low nanomolar concentrations.
The PROTAC degrader, AU-15330, comprising a bait moiety that binds the bromodomain in SMARCA2 and SMARCA4 and a ligand moiety for the von Hippel–Lindau (VHL) ubiquitin ligase.
Treatment of several cell lines with AU-15330 led to time and dose-dependent degradation of SMARCA2, SMARCA4 and PBRM1, exhibited preferential cytotoxicity in enhancer-binding transcription factor-driven cancers.
AR and FOXA1-driven prostate cancer cells to be preferentially sensitive to AU-15330 (IC50<100 nM).
AU-15330 inhibits tumour growth in preclinical models of CRPC and synergizes with enzalutamide.
Inactivation of SWI/SNF ATPase induces a rapid, near-complete and targeted loss of chromatin accessibility at the core-enhancer circuitry of AR, FOXA1, MYC and ERG, thereby attenuating their cancer-promoting transcriptional programs and tempering the enhancer-wired supra-physiologic expression of driver oncogenes.
| M.Wt | 755.939 | |
| Formula | C39H49N9O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2S,4R)-1-((S)-2-(2-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
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1. Lanbo Xiao, et al. Nature. 2022 Jan;601(7893):434-439.
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