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BC-DXI-843

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Chemical Structure| 2421117-98-6 同义名 : -
CAS号 : 2421117-98-6
货号 : A1275415
分子式 : C28H26N4O4S2
纯度 : 99%+
分子量 : 546.66
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(457.32 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AIMP2-DX2, a splicing variant of AIMP2, is up-regulated in lung cancer, possesses oncogenic activity, and results in tumorigenesis. BC-DXI-843 is a potent and selective AIMP2-DX2 inhibitor with an IC50 value of 0.92 μM which is more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. In H460 cells, BC-DXI-843 exhibited dose-dependent inhibition of DX2 protein levels, and it efficiently induced degradation of DX2 at a very low concentration of 1.20 μM. Moreover, BC-DXI-843 demonstrated in vivo efficacy in a tumor xenograft mouse model (H460 cells) at a dosage of 50 mg/kg, suggesting it as a promising lead for development of novel therapeutics targeting AIMP2-DX2 in lung cancer[1].
作用机制 BC-DXI-843 was positioned very close to L80, T82, F116, T117, and K129 and it forms two hydrogen bonds with the hydrophobic pocket via T82 and D52[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.15mL

1.83mL

0.91mL

18.29mL

3.66mL

1.83mL
参考文献

[1]Sivaraman A, Kim DG, Bhattarai D, et al. Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy. J Med Chem. 2020;63(10):5139-5158