STO-609 acetate |
رقم الكتالوجGC15678
One-Click Copy Product Info
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Ca2+-calmodulin-dependent protein kinase kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1173022-21-3
Sample solution is provided at 25 µL, 10mM.
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STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
STO-609 inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/mL, respectively, and also inhibits their autophosphorylation activities. STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC50 value of the compound against CaM-KII is 10 μg/mL. STO-609 inhibits constitutively active CaM-KKα as well as the wild-type enzyme. In transfected HeLa cells, STO-609 suppresses the Ca2+-induced activation of CaM-KIV in a dose-dependent manner. STO-609 significantly reduces the endogenous activity of CaM-KK in SH-SY5Y neuroblastoma cells at a concentration of 1μg/mL (80% inhibitory rate)[1].
References:
[1]. Tokumitsu H, et al. STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J Biol Chem. 2002 May 3;277(18):15813-8.
[2]. Kukimoto-Niino M, et al. Crystal structure of the Ca /calmodulin-dependent protein kinase kinase in complex with the inhibitor STO-609. J Biol Chem. 2011 Jun 24;286(25):22570-9.
Kinase experiment: | CaM-KI (2.5 μg/mL), CaM-KII (0.75 μg/mL), CaM-KIV (9 μg/mL), and mLCK (0.6 μg/mL) are incubated with 40 μM syntide-2 or 50 μM mLC peptide (for mLCK) at 30 °C for 5 min in a solution (25 μL) containing 50 mM HEPES (pH 7.5), 10 mM Mg(Ac)2, 1 mM DTT, 50 μM [γ-32P]ATP (4500 cpm/pmol) with various concentrations of STO-609 (0–10 μg/mL)in Me2SO at a final concentration of 4%) in the presence of 1 mM CaCl2, 2 μM CaM. Protein kinase activity is measured by the phosphocellulose filter method. Specific activities of CaM-KI, CaM-KII, CaM-KIV, and mLCK in the absence of STO-609 are calculated[1]. STO-609 is bound in the ATP-binding pocket of the CaMKKβ KD. The inhibition mechanism of STO-609 is ATP-competitive[2]. |
References: [1]. Tokumitsu H, et al. STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J Biol Chem. 2002 May 3;277(18):15813-8. | |
| Cas No. | 1173022-21-3 | SDF | |
| Chemical Name | 7-oxo-7H-benzo[de]benzo[4,5]imidazo[2,1-a]isoquinoline-3-carboxylic acid compound with acetic acid (1:1) | ||
| Canonical SMILES | O=C1N2C(C3=CC=C(C(O)=O)C4=CC=CC1=C34)=NC5=CC=CC=C25.OC(C)=O | ||
| Formula | C19H10N2O3.C2H4O2 | M.Wt | 374.35 |
| الذوبان | 100 mM NaOH: 10 mg/ml,DMSO: 1 mg/ml | Storage | Desiccate at RT |
| 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 | 2.6713 mL | 13.3565 mL | 26.713 mL |
| 5 mM | 534.3 μL | 2.6713 mL | 5.3426 mL |
| 10 mM | 267.1 μL | 1.3356 mL | 2.6713 mL |
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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 saline, 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
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)