1. Protein Tyrosine Kinase/RTK
  2. Src
  3. Tolimidone

Tolimidone (Synonyms: MLR-1023)

Cat. No.: HY-59047 Purity: 99.98%
Handling Instructions

Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.

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

Tolimidone Chemical Structure

Tolimidone Chemical Structure

CAS No. : 41964-07-2

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.

IC50 & Target

EC50: 63 nM (Lyn kinase)[1]

In Vitro

Incubation of Tolimidone (MLR-1023) with Lyn kinase elicits a repeatable 50% increase in enzyme activity. Tolimidone elicits a concentration-dependent increase in Lyn kinase activation with a 2.3- and 2.1-fold increase achieved at concentrations of 3 and 10 μM, respectively. Inclusion of Tolimidone (100 μM) increases Lyn kinase activity by 3-fold at each ATP concentration tested (Vmax=2601 U/mg). Tolimidone-mediated activation of Lyn kinase increases in proportion to the length of preincubation period in the absence of ATP[1].

In Vivo

Administration of Tolimidone (MLR-1023) (30 mg/kg i.p.) significantly (p<0.05) lowers blood glucose levels to 148 and 158 mg/dL, 30 and 90 min after administration, respectively. Tolimidone significantly increases adipocyte differentiation and adiponectin production by 3.7- and 19-fold, respectively[1]. Tolimidone elicits a dose-dependent potentiation of the insulin response, with a maximal effect observed with a dose level of 30 mg/kg[2].

Clinical Trial
Molecular Weight

202.21

Formula

C₁₁H₁₀N₂O₂

CAS No.

41964-07-2

SMILES

O=C1N=CC(OC2=CC=CC(C)=C2)=CN1

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: 

DMSO : 150 mg/mL (741.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9454 mL 24.7268 mL 49.4535 mL
5 mM 0.9891 mL 4.9454 mL 9.8907 mL
10 mM 0.4945 mL 2.4727 mL 4.9454 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (12.36 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (12.36 mM); Clear solution; Need warming

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

For each kinase assay, Tolimidone (MLR-1023) (10 μM) is preincubated with kinase and fluoroscein-labeled protein substrate. The reaction is initiated with the addition of ATP (at a concentration at or below the Km for each kinase), and the level of fluoroscein phosphopeptide is measured. The assays are conducted in duplicate[1].

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

Cell Assay
[1]

Adipocyte differentiation is assessed in mouse 3T3-L1 cells after 8 days of incubation with Tolimidone (MLR-1023) or rosiglitazone (10 μM). PPAR (α, σ and γ) transactivation studies are conducted in transiently transfected cells containing the appropriate DNA constructs (pGAL4/PPARα, σ or γ) cotransfected with a luciferase reporter vector. Tolimidone or an appropriate reference compound is incubated with transfected cells for 24 h. Luciferase activity is monitored as a measure of PPARα, σ and γ activation[1].

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

Animal Administration
[1]

Male mice, 8 to 10 weeks of age, are used in studies of baseline glucose, glucose tolerance, and insulin levels. Tolimidone (MLR-1023) is administered intraperitoneally at dose volumes of 5 to 10 mL/kg. Blood (5 μL) is acquired from a tail snip and directly applied to a glucose test strip. Blood levels of Tolimidone are measured by liquid chromatography/tandem mass spectrometry, and levels are determined by comparing them with a standard curve of Tolimidone prepared in blood[1].

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

References

Purity: 99.98%

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Keywords:

TolimidoneMLR-1023MLR1023MLR 1023SrcInhibitorinhibitorinhibit

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