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RepSox

E-616452,SJN 2511

RepSox是一种选择性TGFβ/ALK5抑制剂,抑制ATP与ALK5结合以及ALK5自磷酸化时, IC50分别为23 nM和4 nM。

目录号
EY1681
EY1681
EY1681
EY1681
纯度
99.31%
99.31%
99.31%
99.31%
规格
5 mg
10 mg
50 mg
100 mg
原价
605
860
3035
5136
售价
605
860
3035
5136
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    RepSox was found to replace the function of Sox2 to induce reprogramming of iPS cells, via the mechanism of inhibiting TGFβR-1 . MEF cells were treated with RepSox for 3 days, and then it was removed at the time of transduction with Oct4, Klf4, and cMyc. The result showed the TGFβR-1 -associated expression of L-Myc was increased by 5-fold after RepSox treatment . A partially reprogrammed cell line (OKMS 6) was treated with RepSox and performed global gene expression analysis at 10, 24, and 48 hours following the initiation of treatment. The result showed the Id1, Id2 and Id3 gene, repressed by TGFβR-1 signaling, were released from that repression and the expression level was increased. Additionally, other genes responsive for TGFβR-1 signaling were inhibited. It suggested RepSox was able to inhibit TGFβR-1 and suppress the TGFβR-1 downstream signaling.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Gellibert F, et al. J Med Chem, 2004, 47(18), 4494-4506.
    [2] Ichida et al (2009) A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell 5 491.
    [3] Li et al (2009) Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4 16.

    分子式
    C17H13N5
    分子量
    287.32
    CAS号
    446859-33-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    100 mM
    Water
    <1 mg/mL
    Ethanol
    50 mM

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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