Chemical Structure : TEAD PROTAC H122
CAS No.:
TEAD PROTAC H122
Catalog No.: PC-23735Not For Human Use, Lab Use Only.
TEAD PROTAC H122 is a potent, selective TEAD PROTAC degrader with DC50 of 3.0 nM in MSTO-211H cells, shows TEAD1 binding affinity with Ki of 0.3 nM, promotes the degradation of TEAD1, TEAD3, and TEAD4 with similar potency.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TEAD PROTAC H122 is a potent, selective TEAD PROTAC degrader with DC50 of 3.0 nM in MSTO-211H cells, shows TEAD1 binding affinity with Ki of 0.3 nM, promotes the degradation of TEAD1, TEAD3, and TEAD4 with similar potency.
H122 exhibits antiproliferative activity with IC50 of 21.3 and 0.6 nM for MSTO-211H and NCI-H226 cells respectively.
H122 exhibits high affinity for TEAD2, TEAD3, and TEAD4, as evidenced by Ki values that were all below 5 nM。
H122 significantly downregulated the expression of Myc target genes, as highlighted by GSEA analysis.
H122 exhibits robust antitumor efficacy in the MSTO-211H mouse xenograft model.
Physicochemical Properties
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M.Wt
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838.33
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Formula
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C45H45ClFN5O8
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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-((2S)-5-Chloro-2-(((2-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)ethyl)amino)methyl)-2-phenyl-2,3-dihydrobenzofuran-4-yl)-3-fluoro-4-(2-methoxyethoxy)benzamide
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References
1. Lu Y, et al. J Med Chem. 2025 Jan 13. doi: 10.1021/acs.jmedchem.4c02884.
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