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KG-548
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KG-548图片
CAS NO:175205-09-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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].

IC50& Target

HIF-β[1]; HIF-1α[2]

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.
分子量

282.15

性状

Solid

Formula

C9H4F6N4

CAS 号

175205-09-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month