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Compound II757

Chemical Structure : Compound II757

CAS No.:

Compound II757 (II757)

Catalog No.: PC-72716Not For Human Use, Lab Use Only.

Compound II757 (II757) is a potent, cell-active pan-PRMT inhibitor with IC50 of 5-555 nM for eight PRMTs, with the highest inhibition for PRMT4 (IC50=5 nM).

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

    Biological Activity

    Compound II757 (II757) is a potent, cell-active pan-PRMT inhibitor with IC50 of 5-555 nM for eight PRMTs, with the highest inhibition for PRMT4 (IC50=5 nM).
    II757 competitively binds at the SAM binding site of PRMT1, inhibits PRMT1 with an IC50 of 16 nM.
    II757 demonstrated modest inhibition to PRMT3 and PRMT7 (IC50=555 nM).
    II757 (0-100 uM) reduced histone H4 Arg3 asymmetric dimethylation (H4R3me2a) level in HEK293 cells
    II757 displays selectivity over a panel of other methyltransferases (SAHH, NTMT1, SETD7, G9a, NNMT, TbPRMT7 etc.).

    Physicochemical Properties

    M.Wt 537.437
    Formula C20H25BrN8O3S
    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-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)propyl)-3-(3-bromophenyl)guanidine

    References

    1. Iredia D Iyamu, et al. Biomolecules. 2021 Jun 8;11(6):854.

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