| Identification | Back Directory | [Name]
AAK1 inhibitor 1 | [CAS]
2247894-32-0 | [Synonyms]
SGC AAK1 1
AAK1 inhibitor 1
Cyclopropanecarboxamide, N-[6-[3-[[(diethylamino)sulfonyl]amino]phenyl]-1H-indazol-3-yl]-
AAK1,BMP2K,pathway,kinase,Inhibitor,inhibit,associated,SGCAAK11,Wnt,SGC-AAK-1-1,AP2,SGC AAK1 1 | [Molecular Formula]
C21H25N5O3S | [MDL Number]
MFCD31689256 | [MOL File]
2247894-32-0.mol | [Molecular Weight]
427.52 |
| Chemical Properties | Back Directory | [density ]
1.424±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
7.30±0.50(Predicted) | [color ]
Light brown to khaki |
| Hazard Information | Back Directory | [Biological Activity]
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 nMrespectivelyby 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/RIOK1290 nM/RIOK3260 nM/PIP5K1C880 nM/CDKL1960 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-AAK1-1please visit the [storage]
Store at -20°C |
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