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IRAK-1-4 Inhibitor I IRAK-1/4 Inhibitor I

IRAK-1-4 Inhibitor I是白介素受体相关激酶(IRAK)抑制剂,对IRAK-1和IRAK-4的IC50值分别为0.3 μM和0.2 μM。

  • 货号:
    TK0373
  • 规格:
    1mg
    5mg
    10mg
  • 价格:
    0.00

产品参数

CAS No.509093-47-4
生物活性IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
分子式C20H21N5O4
分子量395.41
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder-20°C3 years
溶解性数据DMF : 25 mg/mL (63.23 mM; ultrasonic and warming and heat to 60°C) DMSO : 5 mg/mL (12.65 mM; ultrasonic and adjust pH to 3 with HCl) H2O : < 0.1 mg/mL (insoluble) Ethanol : < 1 mg/mL (insoluble)
体内研究IRAK-1-4 Inhibitor I has IC50 greater than the highest concentration tested (10 μM) against a panel of 27 other kinases, including the most closely homologous (outside of the IRAK family) Lck and pp60. Additionally, IRAK-1-4 Inhibitor I does not show any signs of cytotoxicity in a 72 h proliferation assay in HeLa cells (ED50>30 μM). Significant inhibition of IRAK-1 is observed with IRAK-1-4 Inhibitor I (IRAK-1 IC50=0.3 μM). IRAK-1/4 inhibitor eliminates the LPS-induced increases in Bcl10, NF-κB, and IL-8. IRAK-1/4 mediates LPS-induced IL-8 activation and functions upstream of Bcl10. The LPS-induced increase in Bcl10 declines by 73% (from 5.18±0.22 to 2.36±0.08 ng/mL), and the IL-8 response decline by 60% (from 2.64±0.31 to 1.14±0.08 ng/mL).
文献•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Oncogene. 2020 Sep;39(36):5888-5901. •J Immunol. 2021 Jun 18;ji2100115. •Environ Health. 2020 Aug 1;19(1):87. •Antibiotics. 2020 Jan 17;9(1):33. •Sci Rep. 2016 Jun 8;6:27460.
纯度及产品资料98%