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首页-抗体药物偶连体和PROTACs-PROTAC-SAMHD1 degrader NP12
SAMHD1 degrader NP12

Chemical Structure : SAMHD1 degrader NP12

CAS No.:

SAMHD1 degrader NP12

货号: PC-28651Not For Human Use, Lab Use Only.

SAMHD1 degrader NP12 is a potent, specific SAMHD1 degrader with DC50 of 1.2 uM and Dmax=89% in THP-1 cells (48h).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SAMHD1 degrader NP12 is a potent, specific SAMHD1 degrader with DC50 of 1.2 uM and Dmax=89% in THP-1 cells (48h).
NP12 binds to SAMHD1 in cells and mediates SAMHD1 degradation with low off-target effects.
NP12-mediated SAMHD1 degradation exhibits pathway specificity and that its function depends on the ubiquitin mediated CRL proteasome pathway rather than lysosomal degradation pathway.
NP12 can specifically promote the formation of the SAMHD1-DCAF1 ternary complex, which is a key step in initiating SAMHD1 ubiquitination modification.
NP12 improves cellular sensitivity to the cytotoxic effect of Ara-C.
NP12 delayed pulmonary fibrosis progression and exerted a protective effect on lung tissue in bleomycin-induced pulmonary fibrosis mouse model.

物理化学性质&存储条件

分子量 1080.66
分子式 C54H67ClFN13O8
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

(R)-N-(3-(2-Chloro-4-((4-((1-(4-hydroxybutyl)-4-oxo-4,5-dihydro-1H-pyrazolo­[3,4-d]­pyrimidin-6-yl)­amino)­piperidin-1-yl)­methyl)­phenoxy)­phenyl)-2-(2-(2-(2-(4-(6-((1-(3-fluorophenyl)­piperidin-3-yl)­amino)­pyrimidin-4-yl)­piperazin-1-yl)-2-oxoethoxy)­ethoxy)­ethoxy)­acetamide

参考文献

1. Xing Chen, et al. J Med Chem. 2026 Apr 23;69(8):9363-9385.

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