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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P 2 in the presence of in the presence of [ 33 P]ATP with an IC 50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
In Vitro
APY0201 works differently from anti-IL-12/23 antibodies and acts by inhibiting production of these proinflammatory cytokines with characteristic selectivity over other cytokines, including tumor necrosis factor-alpha (TNF-α). In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibits IL-12p70 and IL-12p40 production, with IC 50 s of 8.4 and 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 shows significant selectivity for the production of IL-12p70 and IL-12p40 over TNF-α, and this selectivity is maintained across species. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:PIKfyve 5.2 nM (IC 50 ) IL-12 IL-23
| Isomeric SMILES | CC1=CC(=CC=C1)/C=N/NC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5 |
|---|---|
| PubChem CID | 56927660 |
| MeSH Entry Terms | APY0201 |
| Molecular Weight | 413.5 |
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