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MRT00033659

MRT00033659 是一种有效的广谱激酶抑制剂,抑制 CK1 (对 CK1δ:IC50=0.9 &#181M) 和 CHK1 (IC50=0.23 &#181M)。MRT00033659 是一种吡唑并吡啶类似物,可以诱导 p53 途径活化和 E2F-1 不稳定。

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MRT00033659的二维码
  • 库存: 现货
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  • 5mg
    ¥1625.00
    1300.00
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  • 10mg
    ¥2725.00
    2180.00
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  • 50mg
    ¥7012.00
    5610.00
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  • 100mg
    ¥10250.00
    8200.00
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  • 货号: ajcx29522
  • CAS: 1401731-54-1
  • 别名:
  • 分子式: C15H14N4O
  • 分子量: 266.3
  • 纯度: >98%
  • 溶解度: DMSO: 83.33 mg/mL (312.92 mM)
  • 储存: Store at -20°C,unstable in solution, ready to use.
  • 库存: 现货

Background

MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation[1].


MRT00033659 (5-40 µM; 48 hours) is sufficient to significantly reduce cell number of 5 µM[1]. MRT00033659 (1-80 µM; 48 hours) induces substantial cell death from 5 µM[1]. MRT00033659 (0.2-80 µM; 48 hours) induces a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM[1]. MRT00033659 does not inhibit p38α MAPK[1]. Cell Viability Assay[1] Cell Line: A375 cells


[1]. Huart AS, et al. A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novelactivator of the p53 pathway. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5578-85.

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