GSK1324726A

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Chemical Structure| 1300031-52-0 同义名 : I-BET726
CAS号 : 1300031-52-0
货号 : A186354
分子式 : C25H23ClN2O3
纯度 : 99%+
分子量 : 434.91
MDL号 : MFCD28144683
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(103.47 mM)，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
生物活性
靶点

  • BET

    BRD2, IC50:31 nM

    BRD4, IC50:22 nM
描述 GSK1324726A works as both a selective BET Bromodomain inhibitor with pIC50 values of 7.4, 7.1, 7 and 7.3 for BRD2, BRD3, BRD4 and BRDT, respectively, and a potent tetrahydroquinoline ApoA1 up-regulator. It inhibited the production of LPS-stimulated IL6 with pIC50 values of 7.3 and 6.4 in PBMC and HWB cells, respectively. Oral administration of GSK1324726A at doses of 3mg/kg and 10mg/kg significantly reduced expression of PAI-1 mRNA in a murine acute LPS challenge model. Intravenous injection with GSK1324726A at dose of 10mg/kg increased the ratio of survival of a murine septic shock model[3].
作用机制 GSK1324726A binds to the acetyl-lysine pocket.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.50mL

2.30mL

1.15mL

22.99mL

4.60mL

2.30mL
参考文献

[1]Gosmini R, Nguyen VL, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31.

[2]Wyce A, Ganji G, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.

[3]Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. PMID: 25249180.