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Chemical Structure : ADH-6
Catalog No.: PC-72589Not For Human Use, Lab Use Only.
ADH-6 is a small molceule that abrogates amyloid formation of aggregation-prone region of mutant p53 DBD with binding Ki of 366 nM (p53 mutant R248W DBD-derived peptide, pR248W).
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ADH-6 is a small molceule that abrogates amyloid formation of aggregation-prone region of mutant p53 DBD with binding Ki of 366 nM (p53 mutant R248W DBD-derived peptide, pR248W).
ADH-6 (5 uM) dissociates mutant p53 aggregates in in MIA PaCa-2 cells, ADH-6 efficiently enters cells to directly interact with and stabilize mutant p53.
ADH-6 causes selective cytotoxicity in cancer cells bearing mutant p53, reduced MIA PaCa-2 cell viability in a concentration-dependent manner, with EC50 of 2.7 and 2.5 uM at 24 and 48 h incubation times, respectively.
ADH-6 decreased cell viability of human cancer cells harboring other aggregation-prone p53 mutants (R248W: COLO 320DM and NCI-H1770; R248Q: HCC70 and OVCAR-3; R175H: LS123; R273H: HT-29 and ARH-77; Y220C: NCI-H748 and NCI-H2342; and R280K: MDA-MB-231).
ADH-6 causes death of cancer cells bearing mutant, but not WT p53, induces transcriptional reactivation of p53.
ADH-6 ((716.4 uM, i.p.) causes regression of mutant p53-bearing tumors in the MIA PaCa-2 xenografts with no adversely effect on body weight, did not significantly alter the amount of WT p53 in MCF-7 xenografts.
| M.Wt | 640.654 | |
| Formula | C29H36N8O9 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. L Palanikumar, et al. Nat Commun. 2021 Jun 25;12(1):3962.
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