Biological Activity
Selective allosteric activator of Lyn kinase (EC50 = 63 nM); displays no significant activity against a range of 47 other kinases, including other Src family kinases such as Fyn, Lck and Src kinase. Reduces blood glucose levels without affecting in vivo insulin secretion. Orally bioavailable.
Compound Libraries
MLR 1023 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 202.21 |
| Formula | C11H10N2O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 41964-07-2 |
| PubChem ID | 39065 |
| InChI Key | HJQILFPVRNHTIG-UHFFFAOYSA-N |
| Smiles | CC1=CC(OC2=CNC(N=C2)=O)=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.22 | 100 | |
| ethanol | 4.04 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 202.21. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.95 mL | 24.73 mL | 49.45 mL |
| 5 mM | 0.99 mL | 4.95 mL | 9.89 mL |
| 10 mM | 0.49 mL | 2.47 mL | 4.95 mL |
| 50 mM | 0.1 mL | 0.49 mL | 0.99 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ochman et al (2012) The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes. J.Pharmacol.Exp.Ther. 342 23 PMID: 22431203
Saporito et al (2012) MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo. J.Pharmacol.Exp.Ther. 342 15 PMID: 22473614
Keywords: MLR 1023, supplier, MLR1023, type, II, diabetes, antidiabetic, hyperglycemia, lyn, kinase, inhibitors, inhibits, selective, Src, Kinases, Src, Kinases, Tocris Bioscience
