p53 Y220C DUBTAC A1

Chemical Structure : p53 Y220C DUBTAC A1

加入收藏

货号: PC-25762Not For Human Use, Lab Use Only.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

p53 Y220C DUBTAC A1 is a bifunctional small molecule p53 Y220C-specific deubiquitinase-targeting chimera (DUBTAC) recruiting both p53 Y220C and the deubiquitinase OTUB1, effectively reactivates and deubiquitinates mutant p53 Y220C in vitro and in vivo.
A1 induced the upregulation of p53 Y220C protein in a dose-dependent manner in Huh7.
A1 could directly interact with p53 Y220C (KD=12.09 µM) in SPR assays.
A1 exhibited mutant-selective engagement with p53 Y220C, does not elevate p53 protein levels in wild-type or other mutant cell lines (R280K, R248W) even at 40 uM.
A1 exhibits potent anti-proliferative efficacy specifically in Y220C-harboring Huh7 cells with IC50 of 1.13 uM.
A1 predominantly removes K48-linked polyubiquitination, whereas K63-linked ubiquitination remains largely unchanged.
A1 (i.v., 40 mg/kg) suppressed Huh7 cells xenograft growth in vivo, upregulated the p53 Y220C protein by approximately 9-fold, significantly increased its downstream targets NOXA, PUMA, and p21.

物理化学性质&存储条件

分子量	721.60
分子式	C34H36IN5O5
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	4-acryloyl-1-(5-(3-(4-(2-hydroxy-3-iodo-5-(3-(phenylamino)prop-1-yn-1-yl)benzyl)piperazin-1-yl)-3-oxopropyl)furan-2-yl)piperazin-2-one

参考文献

1. He C, et al. Angew Chem Int Ed Engl. 2025 Nov 17:e18249.