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

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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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris

Product number: 6528
Product name: SGCAAK11
Purity: ≥98%(HPLC)
Packaging: 5
Price: $95
Updated: 2021/12/16

Tocris

Product number: 6528
Product name: SGCAAK11
Purity: ≥98%(HPLC)
Packaging: 25
Price: $371
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BS168103
Product name: SGC AAK1 1
Packaging: 5mg
Price: $60
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BS168103
Product name: SGC AAK1 1
Packaging: 10mg
Price: $115
Updated: 2021/12/16

ChemScene

Product number: CS-0087586
Product name: SGC-AAK1-1
Packaging: 5mg
Price: $205
Updated: 2021/12/16

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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

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AAK1 inhibitor 1 Suppliers

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2247894-32-0, AAK1 inhibitor 1Related Search:

SGC-GAK-1

AAK1 inhibitor 1

SGC AAK1 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

S C-AAK1-1

SGC-AAK1-1, 10 mM in DMSO

2247894-32-0