Chemical Structure : A5-MMC17
CAS No.:
955533-28-5
A5-MMC17
Catalog No.: PC-25377Not For Human Use, Lab Use Only.
A5-MMC17 is a specific, small molecule allosteric modulator of FBW7 E3 ligase with MST Kd of 45 uM, targets FBW7-pocket G, induces proteasome- and Cullin-RING-dependent c-MYC and c-JUN degradation in cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
A5-MMC17 is a specific, small molecule allosteric modulator of FBW7 E3 ligase with MST Kd of 45 uM, targets FBW7-pocket G, induces proteasome- and Cullin-RING-dependent c-MYC and c-JUN degradation in cells.
binding to FBW7WT showed a Kd of 51 µm and a ΔG of −5.85 kcal mol−1, consistent with initial SPR and MST experiments.
A5-MMC17 (10-250 uM, 2-4 h) caused a consistent dose-dependent reduction in c-MYC protein levels in HEK293 and HCT116 cells, due to proteasomal degradation and the reduction in c-MYC protein levels is also Cullin-RING-dependent.
A5-MMC17 treatment did not affect c-MYC protein levels in HCT116 FBW7-/- cells, indicating it's specificity.
Physicochemical Properties
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M.Wt
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437.40
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Formula
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C20H25BrN2O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-bromo-N-(2-(1-propyl-1,2,3,4-tetrahydroquinolin-6-yl)ethyl)benzenesulfonamide
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References
1. Martínez-Cartró M, et al. Adv Sci (Weinh). 2025 Aug 20:e06068.
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