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DC-TEAD3in03

Chemical Structure : DC-TEAD3in03

CAS No.:

DC-TEAD3in03 (TEAD3 inhibitor)

Catalog No.: PC-73283Not For Human Use, Lab Use Only.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.
    DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.
    DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.
    DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.
    In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

    Physicochemical Properties

    M.Wt 288.391
    Formula C17H24N2O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1-(3-(3-(benzyloxy)propyl)tetrahydropyrimidin-1(2H)-yl)prop-2-en-1-one

    References

    1. Tian Lu, et al. Acta Pharm Sin B. 2021 Oct;11(10):3206-3219.

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