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KG-548

Catalog No. T60539 CAS 175205-09-1

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].

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KG-548, CAS 175205-09-1

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Description

In vitro

Hypoxia-inducible factor (HIF) consists of a heterodimer formed by two basic Helix Loop Helix-Per-ARNT-Sim (bHLH-PAS) subunits, including one of the HIF-α paralogs (HIF-1α, -2α, -3α) and the aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β). KG-548 demonstrates a significant reduction in the formation of the ARNT/CCC complex across coactivators, and disrupts the interactions between ARNT2 PAS-B and TACC3. A dose-dependent disruption by KG-548 of the ARNT PAS-B/TACC3 complex at concentrations of 0 to 2 mM, over 16 hours overnight, was observed, effectively dissociating a 320 μM complex in vitro and in cell lysates, with an IC50 value of 25 μM. Moreover, KG-548 markedly reduces lactate production in glycolysis in FaDu hypopharyngeal carcinoma cells. Western Blot Analysis in HEK293T cell lysates, using concentrations ranging from 0, 5, 50, 100, 250, 500 μM to 1 mM and 2 mM over 16 hours, showed a dose-dependent weakening of the ARNT/TACC3 interaction beginning at 5 μM, and resulted in a significant decrease in protein intensity of ARNT associated with immunoprecipitated TACC3 protein by 82% (500 μM), 59% (1 mM), and 43% (2 mM), respectively.

Molecular Weight	282.15
Formula	C9H4F6N4
CAS No.	175205-09-1

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

KG-548 175205-09-1 inhibitor inhibit

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