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OICR-8268

Chemical Structure : OICR-8268

CAS No.: 3000549-26-5

OICR-8268 (OICR8268)

Catalog No.: PC-20292Not For Human Use, Lab Use Only.

OICR-8268 (OICR8268) is a highly potent, reversible, small molecule ligand of DCAF1 (Vpr binding protein) with SPR KD of 38 nM, a substrate receptor of two distinct E3 ligases (CRL4DCAF1 and EDVP).

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

    Biological Activity

    OICR-8268 (OICR8268) is a highly potent, reversible, small molecule ligand of DCAF1 (Vpr binding protein) with SPR KD of 38 nM, a substrate receptor of two distinct E3 ligases (CRL4DCAF1 and EDVP).
    OICR-8268 exhibits cellular target engagement with EC50 of 10 μM as measured by cellular thermal shift assay (CETSA).
    OICR-8268 shows high affinity for binding to the DCAF1 WDR domain with ITC Kd of 278 nM.
    OICR-8268 is a potent and in-cell active small molecule for the DCAF1 WDR domain.
    DCAF1 is a substrate receptor of two distinct E3 ligases (CRL4DCAF1 and EDVP), plays a critical physiological role in protein degradation, and is considered a drug target for various cancers.

    Physicochemical Properties

    M.Wt 439.24
    Formula C19H14Cl2F2N4O2
    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

    (S)-N-(3-amino-1-(3-chloro-4-fluorophenyl)-3-oxopropyl)-3-(4-chloro-2-fluorophenyl)-1H-pyrazole-4-carboxamide

    References

    1. Li ASM, et al. J Med Chem. 2023 Mar 22. doi: 10.1021/acs.jmedchem.2c02132.

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