Chemical Structure : PT-129
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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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.
分子量 | 936.99 | |
分子式 | C46H48N8O12S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Dong T, et al. J Am Chem Soc. 2024 Dec 22.
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