产品说明书

Bithionol

Print
Chemical Structure| 97-18-7 同义名 : 硫双二氯酚 ;CP 3438;Actamer;Lorothidol;Bitin;NSC 47129;NSC 9872
CAS号 : 97-18-7
货号 : A138799
分子式 : C12H6Cl4O2S
纯度 : 98%
分子量 : 356.052
MDL号 : MFCD00055727
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: 35 mg/mL(98.3 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
动物实验配方：
生物活性
靶点

  • AC

    sAC, IC50:4.0 μM
描述 Bithionol is a potent sAC-specific inhibitor with IC50 value of 4μM[3]. Bithionol inhibited ATP production by working as a classical uncoupler in mitochondria isolated from mouse brain[4].
作用机制 Bithionol binds to the sAC-specific, allosteric binding site for the physiological activator. It induces rearrangements of substrate binding residues and of Arg176, a trigger between the active site and allosteric site.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.04mL

2.81mL

1.40mL

28.09mL

5.62mL

2.81mL
参考文献

[1]Kleinboelting S, Ramos-Espiritu L, et al. Bithionol Potently Inhibits Human Soluble Adenylyl Cyclase through Binding to the Allosteric Activator Site. J Biol Chem. 2016 Apr 29;291(18):9776-84.

[2]Jakobsen E, Lange SC, et al. The inhibitors of soluble adenylate cyclase 2-OHE, KH7, and bithionol compromise mitochondrial ATP production by distinct mechanisms. Biochem Pharmacol. 2018 Sep;155:92-101.

[3]Kleinboelting S, Ramos-Espiritu L, Buck H, Colis L, van den Heuvel J, Glickman JF, Levin LR, Buck J, Steegborn C. Bithionol Potently Inhibits Human Soluble Adenylyl Cyclase through Binding to the Allosteric Activator Site. J Biol Chem. 2016 Apr 29;291(18):9776-84. doi: 10.1074/jbc.M115.708255. Epub 2016 Mar 9. PMID: 26961873; PMCID: PMC4850313.

[4]Jakobsen E, Lange SC, Andersen JV, Desler C, Kihl HF, Hohnholt MC, Stridh MH, Rasmussen LJ, Waagepetersen HS, Bak LK. The inhibitors of soluble adenylate cyclase 2-OHE, KH7, and bithionol compromise mitochondrial ATP production by distinct mechanisms. Biochem Pharmacol. 2018 Sep;155:92-101. doi: 10.1016/j.bcp.2018.06.023. Epub 2018 Jun 22. PMID: 29940175.