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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-OICR-8268
OICR-8268

Chemical Structure : OICR-8268

CAS No.: 3000549-26-5

OICR-8268 (OICR8268)

货号: 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).

规格 价格 库存 数量
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 439.24
    分子式 C19H14Cl2F2N4O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

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

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