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首页-抗体药物偶连体和PROTACs-PROTAC-PT-129
PT-129

Chemical Structure : PT-129

CAS No.:

PT-129 (PT129)

货号: PC-23715Not For Human Use, Lab Use Only.

PT-129 is the first potent, selective, and efficacious G3BP1/2 PROTAC degrader, induces degradation of G3BP1 and G3BP2 with DC50 of 5 and 10 μM respectively in L929 cells, Dmax=95%.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PT-129 is the first potent, selective, and efficacious G3BP1/2 PROTAC degrader, induces degradation of G3BP1 and G3BP2 with DC50 of 5 and 10 μM respectively in L929 cells, Dmax=95%.
PT-129 also reduces G3BP1 levels in other cell lines, including NIH3T3, A549 and KGN cells, with similar DC50 values.
PT-129 (10 uM) inhibits stress granules (SGs) formation by degrading G3BP1 and G3BP2, promoted SG dissolution.
PT-129 downregulates G3BP-associated transcriptome and proteome.
PT-129 inhibits cancer-associated fibroblasts (CAFs) mediated cancer growth and metastasis, inhibits CAF-fostered ATF4 expression and tumor malignancy.
PT-129 suppressed ATF4 intercellular communication in a migracytosis dependent manner.

物理化学性质&存储条件

分子量 936.99
分子式 C46H48N8O12S
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

(2S)-2-((2-(1H-indazol-1-yl)-2-oxoethyl)sulfonamido)-N-(4-(3-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)propanamido)phenyl)-3-phenylpropanamide

参考文献

1. Dong T, et al. J Am Chem Soc. 2024 Dec 22.

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