SML1728

STK16-IN-1

≥98% (HPLC)

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₁₇H₁₂FN₃O
• Número CAS: 1223001-53-3
• Peso molecular: 293.30
• Código UNSPSC: 12352202
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• Formulário: powder
• condição de armazenamento: protect from light
• cor: white to beige
• solubilidade: DMSO: 10 mg/mL, clear (warmed)
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: CC1=CC(N2C(C(C=CN3)=C3N=C4)=C4C=CC2=O)=CC=C1F
• 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)
• chave InChI: WQNRDXHKVSKUPI-UHFFFAOYSA-N

Descrição

Ações bioquímicas/fisiológicas

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.

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.

Informações de segurança

• Pictogramas: GHS07
• Palavra indicadora: Warning
• Frases de perigo: H315,H319
• Declarações de precaução: P264 - P280 - P302 + P352 - P305 + P351 + P338 - P332 + P313 - P337 + P313
• Classificações de perigo: Eye Irrit. 2 - Skin Irrit. 2
• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable