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KG-548

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Chemical Structure| 175205-09-1 同义名 : -
CAS号 : 175205-09-1
货号 : A117262
分子式 : C9H4F6N4
纯度 : 97%
分子量 : 282.145
MDL号 : MFCD06246015
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(372.15 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 KG-548 is an ARNT/TACC3 binding blocker and HIF-1α inhibitor. KG-548 directly interferes with the formation of the ARNT/TACC3 complex by competing with TACC3 for binding to the PAS-B structural domain of ARNT. ARNT is an aryl hydrocarbon receptor nuclear transporter, also known as HIF-β[1][2].At concentrations of 0-250 μM for 16 hours to overnight, KG-548 significantly reduces the formation of the ARNT/CCC complex of both co-activators and also disrupts the ARNT2 PAS-B/TACC3 interaction. And at concentrations of 0-2 mM, KG-548 dose-dependently disassembled (320 μM) ARNT PAS-B/TACC3 complexes in vitro and in cell lysates with an IC50 value of 25 μM[1].KG-548 significantly inhibited lactate production from glycolysis in FaDu cells[2] .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.72mL

3.54mL

1.77mL

35.44mL

7.09mL

3.54mL
参考文献

[1]Guo Y, et al. Regulating the ARNT/TACC3 axis: multiple approaches to manipulating protein/protein interactions with small molecules. ACS Chem Biol. 2013 Mar 15;8(3):626-35.

[2]Kleszcz R, et al. The inhibition of c-MYC transcription factor modulates the expression of glycolytic and glutaminolytic enzymes in FaDu hypopharyngeal carcinoma cells. Adv Clin Exp Med. 2018 Jun;27(6):735-742.