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KG-548 is a dual inhibitor of ARNT/TACC3 and HIF-1α, binding to the β-fold surface involved in HIF-2 dimerization and coactivator recruitment, inhibiting lactate production and useful in cancer research.
Description | KG-548 is a dual inhibitor of ARNT/TACC3 and HIF-1α, binding to the β-fold surface involved in HIF-2 dimerization and coactivator recruitment, inhibiting lactate production and useful in cancer research. |
In vitro | KG-548 (50 μM) significantly inhibited lactic acid production. [1] KG-548 (1 mM) significantly interfered with the binding of ARNT to one or both co-activators. KG-548 (0-2 mM, 16 h) decomposed the (320 μM) ARNT PAS-B/TACC3 complex in a dose-dependent manner in vitro and in cell lysates with an IC50 of 25 μM. [2] |
Alias | KG548 |
Molecular Weight | 282.15 |
Formula | C9H4F6N4 |
Cas No. | 175205-09-1 |
Smiles | FC(F)(F)C1=CC(=CC(=C1)C(F)(F)F)C2=NN=NN2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (283.54 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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