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首页-小分子抑制剂&激动剂-NF-κB Pathway-NF-κB-IT848
IT848

Chemical Structure : IT848

CAS No.: 2102435-79-8

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IT848 (IT-848)

货号: PC-49360Not For Human Use, Lab Use Only.

IT848 (IT-848) is a potent and specific small molecule NF-κB inhibitor, decreases the affinity of NF-κB all five subunits (Rel A, Rel B, c-Rel, p50 and p52) to their DNA binding sites and disrupts downstream biological events.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    IT848 (IT-848) is a potent and specific small molecule NF-κB inhibitor, decreases the affinity of NF-κB all five subunits (Rel A, Rel B, c-Rel, p50 and p52) to their DNA binding sites and disrupts downstream biological events.
    IT848 shows binding affinity to both c-Rel and p50 in the low μM range (Kd of 3.9 and 7.0, respectively).
    IT848 inhibits NF-κB activity through inhibition of DNA binding of all five NF-κB subunits.
    IT848 inhibited proliferation and induced caspase-dependent and independent apoptosis in MM cell lines and patient samples.
    IT848 treatment altered the redox homeostasis of MM cells through depletion of the reduced glutathione pool, selectively inducing oxidative stress in MM but not in healthy cells.
    IT848 significantly improved survival when combined with PD-1 inhibition, shows efficacy of IT848 as single agent and in combination with bortezomib in MM xenograft studies.

    物理化学性质&存储条件

    分子量 348.783
    分子式 C17H17ClN2O4
    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

    9-chloro-8-(hexyloxy)-2H-chromeno[2,3-d]pyrimidine-2,4(3H)-dione

    参考文献

    1. Manpreet Bariana, et al. Mol Cancer Ther. 2022 Oct 3;MCT-22-0257.

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