Biological Activity
MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 369.68 |
| Formula | C16H13ClN4.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 118701007 |
| InChI Key | VRQXEOPUAQLBQI-UHFFFAOYSA-N |
| Smiles | NC1=NC=C(C3=CN=C(N)C=C3)C=C1C2=CC=C(Cl)C=C2.Cl.Cl |
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 | 7.39 | 20 | |
| water | 36.97 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 369.68. 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 | 2.71 mL | 13.53 mL | 27.05 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID: 26617966
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