| Identification | Back Directory | [Name]
STK16-IN-1 | [CAS]
1223001-53-3 | [Synonyms]
STK16-IN-1
STK16 inhibitor 1
STK16-IN-1 >=98% (HPLC)
1-(4-fluoro-3-methylphenyl)-1H-pyrrolo[2,3-h][1,6]naphthyridin-2(7H)-one
1-(4-Fluoro-3-methylphenyl)-1,7-dihydro-2H-pyrrolo[2,3-h]-1,6-naphthyridin-2-one
2H-Pyrrolo[2,3-h]-1,6-naphthyridin-2-one, 1-(4-fluoro-3-methylphenyl)-1,7-dihydro- | [Molecular Formula]
C17H12FN3O | [MDL Number]
MFCD30491884 | [MOL File]
1223001-53-3.mol | [Molecular Weight]
293.3 |
| Chemical Properties | Back Directory | [Boiling point ]
582.3±50.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble | [form ]
powder | [pka]
10.85±0.20(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
STK16-IN-1 is a highly selective STK16 kinase inhibitor. | [Biological Activity]
STK16-IN-1 is a cell-permeable pyrrolonaphthyridinone compound th at acts as an ATP-competitive inhibitor against NAK (Numb Associated Kinase) family serine/threonine kinase STK16 (IC50/substrate = 0.91 μM/4EBP1 and 1.2 μM/DRG1[ATP] = 20 μM) with excellent selectivity over a panel of 378 kinases. Despite its inhibitory potency against PI 3-Ks (IC50 = 1.070.8560.867 μM against p110α/p85αp110δ/p85αp110γ respectively) in cell-free assaysSTK16-IN-1 is ineffective against their cellular activity up to 10 μM concentration. STK16-IN-1 treatment (10 μM for 72 hrs) is shown to cause cell number reduction (~50% in HCT-116 and MCF-7 cultures)as well as increased populations of binucleated cells (~5-fold in MCF-7 culture) and G2/M cells (~7 and 3-fold in HCT-116 and MCF-7 culturesrespectively) in an STK16-dependent manner. A useful tool for elucidating STK16 biological functions. |
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