中文名稱:化合物 KG-548 | 英文名稱:KG-548 |
CAS:175205-09-1 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號(hào): T60539 |
名稱 | KG-548 |
描述 | KG-548 is an ARNT/TACC3 disruptor as well as a HIF-1α inhibitor. KG-548 directly interferes with the formation of the ARNT/TACC3 complex by competitively binding the ARNT PAS-B domain with TACC3. ARNT is the aryl hydrocarbon receptor nuclear translocator which is also known as HIF-β [1][2]. |
體外活性 | 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 IC 50 value 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. |
存儲(chǔ)條件 | Shipping with blue ice. |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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