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STK16-IN-1
产品别名
1223001-53-3
STK16-IN-1
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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C17H12FN3O |
| Molecular weight | 293.30 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | 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. |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| storage condition【储存条件】 | protect from light |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 10 mg/mL, clear (warmed) |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | CC1=CC(N2C(C(C=CN3)=C3N=C4)=C4C=CC2=O)=CC=C1F |
| packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
| Pictograms【象形图】 | GHS07 |
| Signal word【警示用语：】 | Warning |
| Hazard Statements | H315 - H319 |
| Precautionary Statements | P305 + P351 + P338 |
| Hazard Classifications【危险分类】 | Eye Irrit. 2 - Skin Irrit. 2 |
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
