Chemical Structure : PT-129
CAS No.:
PT-129
(PT129)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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936.99
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Formula
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C46H48N8O12S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Dong T, et al. J Am Chem Soc. 2024 Dec 22.
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