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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-A5-MMC17
A5-MMC17

Chemical Structure : A5-MMC17

CAS No.: 955533-28-5

A5-MMC17

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 437.40
分子式 C20H25BrN2O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-bromo-N-(2-(1-propyl-1,2,3,4-tetrahydroquinolin-6-yl)ethyl)benzenesulfonamide

参考文献

1. Martínez-Cartró M, et al. Adv Sci (Weinh). 2025 Aug 20:e06068.

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