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SETDB1 triple Tudor domain

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-173156

    Histone Methyltransferase Cancer
    UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research .
    UNC10013
  • HY-168992

    Histone Methyltransferase Neurological Disease Cancer
    UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases .
    UNC6535
  • HY-168992A

    Histone Methyltransferase Others
    UNC6535 TFA is a covalent ligand targeting the triple Tudor domain (3TD) of SETDB1. UNC6535 TFA reversibly binds to the aromatic cages of both TD2 and TD3 within SETDB1 3TD simultaneously, weakly inhibits the methyltransferase activity of SETDB1, and displaces the H3K9Me2K14Ac peptide from SETDB1 3TD .
    UNC6535 TFA

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