Biological Activity
Potent and selective Lck and Src inhibitor (IC50 values are 2 and 6 nM respectively). Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases. Supports self-renewal of naive hESCs in combination with PD 0325901, CHIR 99021 and SB 590885.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of WH-4-023 is reviewed on the chemical probes website.
Compound Libraries
WH-4-023 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 568.67 |
| Formula | C32H36N6O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 837422-57-8 |
| PubChem ID | 11844351 |
| InChI Key | NBTNHSGBRGTFJS-UHFFFAOYSA-N |
| Smiles | O=C(OC5=C(C)C=CC=C5C)N(C4=CC=C(OC)C=C4OC)C1=NC(NC(C=C3)=CC=C3N2CCN(C)CC2)=NC=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 | 56.87 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 568.67. 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 | 1.76 mL | 8.79 mL | 17.58 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.76 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Theunissen et al (2014) Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell 15 471 PMID: 25090446
Clark et al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986 PMID: 23033494
Martin et al (2006) Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J.Med.Chem. 49 4981 PMID: 16884310
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