SGC-AAK1-1

Name: SGC-AAK1-1
Brand: MedChemExpress
SKU: HY-123940
Rating: 4.5 (1 reviews)

Cat. No.: HY-123940 Purity: 98.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC₅₀ of 270 nM and a K_i of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1.

For research use only. We do not sell to patients.

SGC-AAK1-1 Chemical Structure

CAS No. : 2247894-32-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

IC50: 270 nM (AAK1)^[1].
Ki: 9 nM (AAK1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 10000 nM Compound: 25; SGC-AAK1-1	Inhibition of tracer K5 binding to N-terminal nano luciferase-fused GAK (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay Inhibition of tracer K5 binding to N-terminal nano luciferase-fused GAK (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay	[PMID: 32184967]
HEK293	IC₅₀	> 10000 nM Compound: 25; SGC-AAK1-1	Inhibition of tracer K5 binding to N-terminal nano luciferase-fused STK16 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay Inhibition of tracer K5 binding to N-terminal nano luciferase-fused STK16 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay	[PMID: 32184967]
HEK293	IC₅₀	2800 nM Compound: 25; SGC-AAK1-1	Inhibition of tracer K5 binding to N-terminal nano luciferase-fused BMP2K (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay Inhibition of tracer K5 binding to N-terminal nano luciferase-fused BMP2K (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay	[PMID: 32184967]
HEK293	IC₅₀	770 nM Compound: 25; SGC-AAK1-1	Inhibition of tracer K5 binding to N-terminal nano luciferase-fused AAK1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay Inhibition of tracer K5 binding to N-terminal nano luciferase-fused AAK1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition and measured within 10 mins by NanoBRET assay	[PMID: 32184967]

In Vitro

SGC-AAK1-1 (1.25 μM) significantly reduces phosphorylation of AP2M1 (T156) and activates WNT-driven BAR activity compared in a dose-dependent manner in HT1080 cells^[1].
SGC-AAK1-1 blocks AAK1 kinase activity, resulting in increased β-catenin protein stability and β-catenin-dependent transcription^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

427.52

Formula

C₂₁H₂₅N₅O₃S

CAS No.

2247894-32-0

Appearance

Solid

Color

Light brown to khaki

SMILES

O=C(C1CC1)NC2=NNC3=C2C=CC(C4=CC=CC(NS(=O)(N(CC)CC)=O)=C4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (116.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3391 mL	11.6954 mL	23.3907 mL
5 mM	0.4678 mL	2.3391 mL	4.6781 mL
10 mM	0.2339 mL	1.1695 mL	2.3391 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.93%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (249 KB) LCMS (97 KB) Elemental Analysis Report (107 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3391 mL	11.6954 mL	23.3907 mL	58.4768 mL
	5 mM	0.4678 mL	2.3391 mL	4.6781 mL	11.6954 mL
	10 mM	0.2339 mL	1.1695 mL	2.3391 mL	5.8477 mL
	15 mM	0.1559 mL	0.7797 mL	1.5594 mL	3.8985 mL
	20 mM	0.1170 mL	0.5848 mL	1.1695 mL	2.9238 mL
	25 mM	0.0936 mL	0.4678 mL	0.9356 mL	2.3391 mL
	30 mM	0.0780 mL	0.3898 mL	0.7797 mL	1.9492 mL
	40 mM	0.0585 mL	0.2924 mL	0.5848 mL	1.4619 mL
	50 mM	0.0468 mL	0.2339 mL	0.4678 mL	1.1695 mL
	60 mM	0.0390 mL	0.1949 mL	0.3898 mL	0.9746 mL
	80 mM	0.0292 mL	0.1462 mL	0.2924 mL	0.7310 mL
	100 mM	0.0234 mL	0.1170 mL	0.2339 mL	0.5848 mL

SGC-AAK1-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGC-AAK1-12247894-32-0AAK1Adaptor-associated Kinase 1AP2-associated kinase 1AP2associatedkinaseBMP2KWntpathwayInhibitorinhibitorinhibit

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SGC-AAK1-1

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Complete Stock Solution Preparation Table

SGC-AAK1-1 Related Classifications

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