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OICR-9429

OICR-9429 是一个新颖的相互作用的小分子Wdr5-MLL 拮抗剂，IC50是 5 uM，在体外抑制急性髓性白血病细胞。

CAS号

1801787-56-3

分子式

C29H32F3N5O3

主要靶点

JAK|Histone Methyltransferase

仅限科研使用

Cat No : CM04577

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Synonyms

OICR 9429

验证数据展示

  • CAS No.: 1801787-56-3

    OICR-9429
    CAS#: 1801787-56-3

产品信息

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

CAS号 1801787-56-3
分子式 C29H32F3N5O3
主要靶点 JAK|Histone Methyltransferase
主要通路 血管生成|JAK/STAT信号通路|表观遗传|干细胞
分子量 555.59
纯度 99.74%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 OICR 9429

靶点活性

WDR5:93 nM(Kd)

体外活性

OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM)[1].

溶解度

DMSO:38 mg/mL (68.39 mM),H2O:<1 mg/mL,Ethanol:12 mg/mL(21.6 mM)

细胞实验

20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.(Only for Reference)

参考文献

1.Grebien F, et al. Nat Chem Biol. 2015, 11(8):571-8.

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