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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-CG223
CG223

Chemical Structure : CG223

CAS No.: 1629873-79-5

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CG223 (CG14223)

货号: PC-20163Not For Human Use, Lab Use Only.

CG223 (CG14223) is a potent and specific inhibitor of BET proteins with Kd of 45 nM for the C-terminal bromodomain of BRD3 (i.e. BRD3(2)) to 370 nM for the N-terminal bromodomain of BRDT (i.e. BRDT(1)).

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

    生物&药学活性

    CG223 (CG14223) is a potent and specific inhibitor of BET proteins with Kd of 45 nM for the C-terminal bromodomain of BRD3 (i.e. BRD3(2)) to 370 nM for the N-terminal bromodomain of BRDT (i.e. BRDT(1)).
    CG223 shows Ki values of 200 nM and 120 nM for BRD4(1) and BRD4(2), respectively, and Kd value of 34 nM for BRD4(1,2).
    CG223 significantly stronger binding compared to the binding to the bromodomains of BRD9, CBP, and p300, underscoring the specificity of CG223 to BET proteins.
    CG223 (50 mg/kg) suppressed bleomycin-induced pulmonary fibrosis in mice through the suppression of pro-fibrotic proteins Thbs1, Itgb3, and Acta2 gene expression in lung fibroblasts.
    CG223 potently inhibited the expression of fibrillar collagens (collagen type I and III) as well as α-SMA in the MyoF system in dose-dependent manner.

    物理化学性质&存储条件

    分子量 359.43
    分子式 C22H21N3O2
    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

    4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)-1-methylquinolin-2(1H)-one

    参考文献

    1. Shunya Kaneshita, et al. Pulm Pharmacol Ther. 2021 Oct;70:102057.

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