| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
SGC-AAK1-1N selectively targets AP2-Associated Kinase 1 (AAK1), an enzyme that phosphorylates the micro2 subunit of the Adaptor Protein complex 2 (AP-2), regulating clathrin-mediated endocytosis.
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|---|---|
| ln Vitro |
Detailed in vitro potency is characterized by the IC50 value of 1.8 microM against AAK1 enzymatic activity. It demonstrates selectivity for AAK1 over other related kinases, making it a specific chemical probe for studying AAK1 function in cellular processes.
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| ln Vivo |
Dedicated in vivo efficacy studies for SGC-AAK1-1N are not extensively documented in standard profiles. As a selective chemical probe, its primary application is in cell-based mechanistic studies rather than in vivo efficacy models.
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| Enzyme Assay |
Recombinant AAK1 enzyme is incubated with a peptide substrate and gamma-33P-ATP. The reaction is terminated, and the phosphorylated substrate is captured on filter papers. Radioactivity is quantified by scintillation counting in the presence or absence of SGC-AAK1-1N.
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| Cell Assay |
Cells are treated with SGC-AAK1-1N at various concentrations. To assess on-target activity, the phosphorylation status of the AAK1 substrate (micro2 subunit of AP-2) is measured by Western blot using a phospho-specific antibody. Endocytosis assays can be performed to assess functional impact.
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| Animal Protocol |
In vivo protocols for SGC-AAK1-1N are not standard. If used in animal models, the compound would be dissolved in a suitable vehicle (e.g., DMSO/PEG300/saline) and administered via intraperitoneal injection. Tissues would be harvested for downstream analysis of AAK1 target engagement.
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| ADME/Pharmacokinetics |
Detailed PK parameters for SGC-AAK1-1N are not extensively documented. As a research compound typically used in cellular assays, extensive in vivo PK profiling is not a primary focus. Standard oral bioavailability is not reported.
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| Toxicity/Toxicokinetics |
Toxicological data for SGC-AAK1-1N is not available in standard profiles. As a research chemical, it is not intended for clinical development, and comprehensive toxicology studies have not been performed. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
SGC-AAK1-1N is part of the Structural Genomics Consortium (SGC) library of chemical probes. It is designed to be a high-quality, selective tool for biological research to investigate the role of AAK1 in neurological disorders and viral infections. It is not an approved drug.
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| Molecular Formula |
C20H22N4O3S
|
|---|---|
| Molecular Weight |
398.478682994843
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| Exact Mass |
398.141
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| CAS # |
2242913-80-8
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| PubChem CID |
146121078
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
673
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C(=O)NC1=NNC2=C1C=CC(=C2)C3=CC(=CC=C3)NS(=O)(=O)C4CC4
|
| InChi Key |
RAIAORGFMNXPOV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N4O3S/c1-12(2)20(25)21-19-17-9-6-14(11-18(17)22-23-19)13-4-3-5-15(10-13)24-28(26,27)16-7-8-16/h3-6,9-12,16,24H,7-8H2,1-2H3,(H2,21,22,23,25)
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| Chemical Name |
N-[6-[3-(cyclopropylsulfonylamino)phenyl]-1H-indazol-3-yl]-2-methylpropanamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5095 mL | 12.5477 mL | 25.0954 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0191 mL | |
| 10 mM | 0.2510 mL | 1.2548 mL | 2.5095 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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