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STO-609 CaMK inhibitor

Name: STO-609
Brand: Selleck Chemicals
SKU: S8274
Rating: 5 (23 reviews)

Cat.No.S8274

STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that 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. This compound inhibits AMPKK activity and inhibits autophagy.

Chemical Structure

Molecular Weight: 314.29

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Quality Control

Batch: Purity: 99.90%

99.90

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other CaMK Inhibitors	KN-93 Phosphate KN-93 KN-62 NH125 KN-92 phosphate KN-93 hydrochloride

Chemical Information, Storage & Stability

Molecular Weight	314.29	Formula	C₁₉H₁₀N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	52029-86-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C2C(=C1)N=C3N2C(=O)C4=CC=CC5=C(C=CC3=C54)C(=O)O

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (6.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.075mg/ml (0.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 1.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Mechanism of Action

Targets/IC₅₀/Ki	AMPK CaM-KKβ (Cell-free assay) 47 nM(Ki) CaM-KKα (Cell-free assay) 0.25 μM(Ki)
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. This compound is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV). In transfected HeLa cells, this chemical suppresses the Ca²⁺-induced activation of CaM-KIV in a dose-dependent manner. It can permeate cells and is a competitive inhibitor of ATP.
In vivo	In vivo administration of STO-609 results in increased osteoblasts and diminished osteoclasts, conferring significant protection from ovariectomy (OVX)-induced osteoporosis in adult mice. ICV administration of this compound in vivo did not affect the counterregulatory responses to neuroglucopenia and AMPK activation induced by glucopenia.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11867640/ [2] https://pubmed.ncbi.nlm.nih.gov/23408651/ [3] https://pubmed.ncbi.nlm.nih.gov/17687000/ [4] https://pubmed.ncbi.nlm.nih.gov/15980064/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-AMPK / AMPK p-AKT / AKT / p-ERK / ERK		27158402
Growth inhibition assay	Cell viability		27158402

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Handling Instructions

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