Synonym: 1-(4-Fluoro-3-methylphenyl)-1,7-dihydro-2H-pyrrolo[2,3-h]-1,6-naphthyridin-2-one; 1-(4-Fluoro-3-methylphenyl)-1H-pyrrolo[2,3-h][1,6]naphthyridin-2(7H)-one
CAS Number: 1223001-53-3
Empirical Formula (Hill Notation): C17H12FN3O
Molecular Weight: 293.30
Linear Formula: C17H12FN3O
Product Type: Chemical
| assay |
≥98% (HPLC) |
| color |
white to beige |
| form |
powder |
| InChI |
1S/C17H12FN3O/c1-10-8-12(3-4-14(10)18)21-15(22)5-2-11-9-20-17-13(16(11)21)6-7-19-17/h2-9H,1H3,(H,19,20) |
| InChI key |
WQNRDXHKVSKUPI-UHFFFAOYSA-N |
| Quality Level |
100  |
| SMILES string |
CC1=CC(N2C(C(C=CN3)=C3N=C4)=C4C=CC2=O)=CC=C1F |
| solubility |
DMSO: 10 mg/mL, clear (warmed) |
| storage condition |
protect from light |
| storage temp. |
2-8°C |
| Biochem/physiol Actions: |
STK16-IN-1 is a cell-permeable pyrrolonaphthyridinone compound that 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 = 1.07, 0.856, 0.867 μM against p110α/p85α, p110σ/p85α, p110γ , respectively) in cell-free assays, STK16-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 cultures, respectively) in an STK16-dependent manner. A useful tool for elucidating STK16 biological functions. |
| Biochem/physiol Actions: |
STK16-IN-1 is a cell-permeable pyrrolonaphthyridinone compound that acts as an ATP-competitive inhibitor against NAK family serine/threonine kinase STK16 with excellent selectivity. |
| Packaging: |
5, 25 mg in glass bottle |
| Symbol |
 GHS07 |
| Signal word |
Warning |
| Hazard statements |
H315 - H319 |
| Precautionary statements |
P305 + P351 + P338 |
| RIDADR |
NONH for all modes of transport |
| WGK Germany |
WGK 3 |
| Flash Point(F) |
Not applicable |
| Flash Point(C) |
Not applicable |
| Purity |
≥98% (HPLC) |
| Storage Temp. |
2-8°C |
| UNSPSC |
12352202 |
