KG-548 是一个ARNT/TACC3干扰子和HIF-1α抑制剂。KG-548 通过与 TACC3 竞争结合到 ARNT 的 PAS-B 结构域，而直接干扰ARNT/TACC3复合体的形成。ARNT是芳基烃受体核转位器，也称为 HIF-β。
| 生物活性 | KG-548 is anARNT/TACC3disruptor and aHIF-1αinhibitor. KG-548 directly interferes withARNT/TACC3complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is thearyl hydrocarbon receptornuclear translocator, also known asHIF-β[1][2]. |
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体外研究
(In Vitro) | HIF is a heterodimer of two bHLH-PAS (basic Helix Loop Helix-Per-ARNT-Sim) subunits, including a HIF-α paralog (HIF-1α, -2α, -3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β)[1].
KG-548 (0-250 μM; 16 h for over night) exhibits the great reduction of ARNT/CCC complex formation for both coactivators, and also disrupts ARNT2 PAS-B/TACC3 interactions[1].
KG-548 (0-2 mM; 16 h for over night) dose-dependently breaks up the (320 μM) ARNT PAS-B/TACC3 complex in vitro and in cell lysate with an IC50value of 25 μM[1].
KG-548 significantly inhibits lactate production of glycolysis on in FaDu hypopharyngeal carcinoma cells[2].
Western Blot Analysis[1] | Cell Line: | HEK293T cell lysates | | Concentration: | 0, 5, 50, 100, 250, 500 μM and 1 mM, 2 mM | | Incubation Time: | 16 hours | | Result: | Weakened the ARNT/TACC3 interaction from 5 μM to 500 μM dose-dependently, and decreased the protein intense of ARNT associated with immunoprecipitated TACC3 protein by 82% (500 μM), 59% (1 mM), 43% (2 mM), respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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