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Organic compounds that consists entirely of hydrogen and carbon elements usually organized in a chain; some may have a cyclic structure. Includes hydrocarbons that have additional functional groups such as aromatic rings.
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BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 nM for human PI4KIIIβ and 3.5 nM for the *Plasmodium* variant of PI4KIIIβ. For research use only.
Treatment with 0.5 μM of either KAI407 or BQR695 causes GFP-PHOsh2 to redistribute to the parasite plasma membrane, consistent with depletion of intracellular PI4P upon inhibition of PfPI4K function.
BQR695 shows no evidence of toxicity against mature red blood cells (RBCs).
It induces a schizont-stage arrest indistinguishable from that observed in imidazopyrazine-treated parasites and exhibits cross-resistance with the imidazopyrazine-resistant lines.
DMSO: 50 mg/mL (141.89 mM; requires ultrasonic; hygroscopic DMSO has a significant impact on solubility, use newly opened DMSO).
Powder: -20°C for 3 years, 4°C for 2 years.
In solvent: -80°C for 2 years, -20°C for 1 year.
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ETC-159 is a potent, orally available PORCN inhibitor that inhibits β-catenin reporter activity with an IC50 of 2.9 nM. It is intended for research use only.
Inhibits β-catenin reporter activity
Potent and orally available PORCN inhibitor
Active in multiple cancer models with high Wnt signaling
Efficacious in colorectal cancers with R-spondin translocations
Good oral pharmacokinetics in mice with 100% oral bioavailability
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