SML2219

SGC-AAK1-1

≥98% (HPLC)

• Sinonimo/i: N-(6-(3-(N,N-Diethylsulfamoylamino)phenyl)-1H-indazol-3-yl)cyclopropanecarboxamide
• Formula empirica (notazione di Hill): C₂₁H₂₅N₅O₃S
• Numero CAS: 2247894-32-0
• Peso molecolare: 427.52
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Forma fisica: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: CCN(CC)S(NC1=CC=CC(C2=CC(NN=C3NC(C4CC4)=O)=C3C=C2)=C1)(=O)=O

Descrizione

Azioni biochim/fisiol

SGC-AAK1-1 is an ATP-competitive kinase inhibitor against AP2-associated protein kinase 1/AAK1 and BMP-2-inducible protein kinase/BIKE/BMP2K (Ki = 9.1 & 17 nM, respectively, by ATP site fluorescent tracer displacement assay; AAK1 IC50 = 270 nM by coupled enzyme assay). SGC-AAK1-1 downregulates cellular AP2M1 Thr156 phosphorylation level in a dose-dependent manner (ECmax ∼12.5 μM) without detectable cytotoxicity. Selectivity profiling identifies only 5 additional kinases among a panel of ∼400 with >50% inhibition by 1 μM SGC-AAK1-1 (KD = 72 nM/RIOK1, 290 nM/RIOK3, 260 nM/PIP5K1C, 880 nM/CDKL1, 960 nM/MYLK2 by DiscoverX KINOMEscan). SGC-AAK1-1N is a structure analog and the recommended negative control (IC50 = 11 μM by AAK1 activity assay; KD = 8.8 μM/AAK1 & >10 μM/BIKE vs. KD = 26 nM/AAK1 & 930 nM/BIKE with SGC-AAK1-1 by DiscoverX). For characterization details of SGC-AAK1-1, please visit the SGC-AAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.

SGC-AAK1-1N is the negative control for the active probe, SGC-AAK1-1. SGC-AAK1-1N is available from Sigma. To learn more about and purchase SGC-AAK1-1N, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc

Caratteristiche e vantaggi

SGC-AAK1-1 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable