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

STO-609 

Cat. No.: HY-19805 Purity: ≥98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

STO-609 Chemical Structure

STO-609 Chemical Structure

CAS No. : 52029-86-4

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10 mg USD 144 In-stock
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25 mg USD 288 In-stock
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50 mg USD 528 In-stock
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100 mg USD 888 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

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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].

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

Molecular Weight

314.29

Formula

C₁₉H₁₀N₂O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

DMSO : 1 mg/mL (3.18 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.3182 mL 1.5909 mL 3.1818 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  50% PEG300    50% saline

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

  • 2.

    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

  • 3.

    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

*All of the co-solvents are provided by MCE.
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
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Product Name:
STO-609
Cat. No.:
HY-19805
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