KG-548
CAS No. : 175205-09-1
| Size | Price | Stock |
|---|---|---|
| 250mg | $22 | In-stock |
| 1g | $27 | In-stock |
| 5g | $93 | In-stock |
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| Cat. No. : | HY-120087 |
| M.Wt: | 282.15 |
| Formula: | C9H4F6N4 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β[1][2].
IC50 & Target:HIF-β[1]; HIF-1α[2]
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 IC50 value of 25 μM[1].
KG-548 significantly inhibits lactate production of glycolysis in FaDu hypopharyngeal carcinoma cells[2].
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