Compound 43 TAO Kinase Inhibitor |
| カタログ番号GC43304 |
コンパウンド43は、千一種類のアミノ酸キナーゼTAOK1およびTAOK2のATP競合阻害剤であり、それぞれのIC50値は11nMおよび15nMです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 850467-66-2
Sample solution is provided at 25 µL, 10mM.
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Compound 43 TAO kinase inhibitor is an ATP-competitive inhibitor of the thousand-and-one amino acid kinases TAOK1 and TAOK2 (IC50s = 11 and 15 nM, respectively). It is selective for TAOK1 and TAOK2 over 62 kinases in a panel, but does inhibit TAOK3 by 87% and seven additional kinases by 21-52%. Compound 43 TAO kinase inhibitor inhibits proliferation of SK-BR-3, BT-549, and MCF-7 cells by 94, 82, and 46%, respectively, at a concentration of 10 µM. It reduces tau phosphorylation by TAOK2 at residues S262/S356 and S202/T205/S208 when used at concentrations ranging from 5 to 60 µM in a kinase assay and at residues S202/T205/S208 when used at concentrations of 5, 10, and 30 µM in HEK293 cells. Compound 43 TAO kinase inhibitor reduces tau phosphorylation of residues T123 and T427, which are phosphorylated by TAOK1 and TAOK2 in vitro and have been identified in tangles in Alzheimer's disease brain tissue. It also reduces tau phosphorylation in cortical neurons in a transgenic mouse model of tauopathy and in induced pluripotent stem cell-derived neurons from patients with frontotemporal lobar degeneration.
| Cas No. | 850467-66-2 | SDF | |
| Canonical SMILES | O=C(NCC(NC1CCCC2=C1C=CC=C2)=O)C(C=C3)=CC=C3C4=CC=CC=C4 | ||
| Formula | C25H24N2O2 | M.Wt | 384.5 |
| 溶解度 | DMSO: 100 mM,Ethanol: 20 mM | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6008 mL | 13.0039 mL | 26.0078 mL |
| 5 mM | 0.5202 mL | 2.6008 mL | 5.2016 mL |
| 10 mM | 0.2601 mL | 1.3004 mL | 2.6008 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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