2. Neuronal Signaling PI3K/Akt/mTOR Epigenetics Autophagy
  3. CaMK AMPK Autophagy
  4. STO-609

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.

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STO-609 Chemical Structure

STO-609 Chemical Structure

CAS No. : 52029-86-4

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of STO-609:

STO-609 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

Ki: 80 ng/mL (CaM-KKα), 15 ng/mL (CaM-KKβ)[1]
In Vitro

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].

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

STO-609 Related Antibodies
Molecular Weight

314.29

Formula

C19H10N2O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C2C3=C(C4=NC5=CC=CC=C5N4C(C3=CC=C2)=O)C=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (95.45 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 5.56 mg/mL (17.69 mM; Need ultrasonic)

H2O : 0.1 mg/mL (0.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1818 mL 15.9089 mL 31.8177 mL
5 mM 0.6364 mL 3.1818 mL 6.3635 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 0.1 mg/mL (0.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.1 mg/mL (0.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 0.5 mg/mL (1.59 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
References
Kinase Assay
[2]

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].

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

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF / DMSO 1 mM 3.1818 mL 15.9089 mL 31.8177 mL 79.5444 mL
5 mM 0.6364 mL 3.1818 mL 6.3635 mL 15.9089 mL
10 mM 0.3182 mL 1.5909 mL 3.1818 mL 7.9544 mL
15 mM 0.2121 mL 1.0606 mL 2.1212 mL 5.3030 mL
DMSO 20 mM 0.1591 mL 0.7954 mL 1.5909 mL 3.9772 mL
25 mM 0.1273 mL 0.6364 mL 1.2727 mL 3.1818 mL
30 mM 0.1061 mL 0.5303 mL 1.0606 mL 2.6515 mL
40 mM 0.0795 mL 0.3977 mL 0.7954 mL 1.9886 mL
50 mM 0.0636 mL 0.3182 mL 0.6364 mL 1.5909 mL
60 mM 0.0530 mL 0.2651 mL 0.5303 mL 1.3257 mL
80 mM 0.0398 mL 0.1989 mL 0.3977 mL 0.9943 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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STO-609 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:

STO-60952029-86-4STO609STO 609CaMKAMPKAutophagyCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesAMP-activated protein kinaseInhibitorinhibitorinhibit

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