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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-STAT-W1046
W1046

Chemical Structure : W1046

CAS No.: 2816059-41-1

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W1046 (W 1046)

货号: PC-20066Not For Human Use, Lab Use Only.

W1046 is a potent and selective STAT3 inhibitor, decreases the expression of VISTA at mRNA and protein level and inhibits proliferation and survival in AML cells.

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

    生物&药学活性

    W1046 is a potent and selective STAT3 inhibitor, decreases the expression of VISTA at mRNA and protein level and inhibits proliferation and survival in AML cells.
    W1046 occupied the pivotal core of SH2 domain and elevated thermal stability of STAT3 protein.
    W1046 significantly decreased the expression of VISTA at mRNA and protein level in AML cells.
    W1046 significantly inhibited AML cells with hyperactive STAT3 (MOLM-13, IC50=1.85 uM) but was lacked of sensitivity in MCF-7 cells with low STAT3 activation (IC50>15 uM) and in MOLM-13 cells with STAT3 deletion by CRISPR-Cas9.
    W1046 displayed no or slight effect on the phosphorylation of STAT1, STAT5, and upstream kinase JAK2.
    W1046 significantly inhibited proliferation and induced apoptosis both in AML cells lines and in primary AML patient samples.
    W1046 remarkedly suppressed leukemia aggression, reduced leukemia burden and prolonged the survival of leukemia mice dosage-dependently.
    Combination of VISTA mAb and STAT3 inhibitor displayed potent anti-leukemia effect in xenograft mouse models with MOLM-13-EGFP/Luc cells.

    物理化学性质&存储条件

    分子量 610.40
    分子式 C28H28BF5N2O5S
    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-(N-(4-cyclohexylbenzyl)-2-((2,3,4,5,6-pentafluoro-N-methylphenyl)sulfonamido)acetamido)phenyl)boronic acid

    参考文献

    1. Mo J, et al. J Hematol Oncol. 2023 Feb 27;16(1):15.

    2. Deng L, et al. Boronic acid: a novel pharmacophore targeting src homology 2 (SH2) domain of STAT3. J Med Chem, 2022.

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