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.
| Molecular Weight | 293.3 |
| Formula | C17H12FN3O |
| CAS Number | 1223001-53-3 |
| Solubility (25°C) | DMSO: 10 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Feiyang Liu, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor
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