AAK1 inhibitor 1
- Product Name
- AAK1 inhibitor 1
- CAS No.
- 2247894-32-0
- Chemical Name
- AAK1 inhibitor 1
- Synonyms
- S C-AAK1-1;SGC AAK1 1;AAK1 inhibitor 1;SGC-AAK1-1, 10 mM in DMSO;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
- CBNumber
- CB65867501
- Molecular Formula
- C21H25N5O3S
- Formula Weight
- 427.52
- MOL File
- 2247894-32-0.mol
AAK1 inhibitor 1 Property
- Density
- 1.424±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 7.30±0.50(Predicted)
- form
- Solid
- color
- Light brown to khaki
N-Bromosuccinimide Price
- Product number
- 6528
- Product name
- SGCAAK11
- Purity
- ≥98%(HPLC)
- Packaging
- 5
- Price
- $95
- Updated
- 2021/12/16
- Product number
- 6528
- Product name
- SGCAAK11
- Purity
- ≥98%(HPLC)
- Packaging
- 25
- Price
- $371
- Updated
- 2021/12/16
- Product number
- BS168103
- Product name
- SGC AAK1 1
- Packaging
- 5mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- BS168103
- Product name
- SGC AAK1 1
- Packaging
- 10mg
- Price
- $115
- Updated
- 2021/12/16
- Product number
- CS-0087586
- Product name
- SGC-AAK1-1
- Packaging
- 5mg
- Price
- $205
- Updated
- 2021/12/16
AAK1 inhibitor 1 Chemical Properties,Usage,Production
Uses
SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1[1].
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 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
storage
Store at -20°C
References
[1] Agajanian MJ, et al. WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop. Cell Rep. 2019 Jan 2;26(1):79-93.e8. DOI:10.1016/j.celrep.2018.12.023
AAK1 inhibitor 1 Preparation Products And Raw materials
Raw materials
Preparation Products
AAK1 inhibitor 1 Suppliers
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