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Submit ReviewWH-4-023
Description: Potent and selective Lck and Src inhibitor; also inhibits SIK
Alternative Names: KIN112
Chemical Name: 2,6-Dimethylphenyl-N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]carbamate
Purity: ≥98% (HPLC)
Biological Activity for WH-4-023
WH-4-023 is a 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 for WH-4-023
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 for WH-4-023
WH-4-023 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for WH-4-023
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for WH-4-023
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.87 | 100 |
Preparing Stock Solutions for WH-4-023
The following data is based on the product molecular weight 568.67. Batch specific molecular weights may vary from batch to batch due to the degree 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 for WH-4-023
References for WH-4-023
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for WH-4-023, please let us know.
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Keywords: WH-4-023, WH-4-023 supplier, Potent, selective, Lck, Src, inhibitors, inhibits, self-renewal, ESC, lymphocyte, specific, kinase, salt, inducible, SIK, KIN112, Kinases, Other, Stem, Cell, Proliferation, 5413, Tocris Bioscience
2 Citations for WH-4-023
Citations are publications that use Tocris products. Selected citations for WH-4-023 include:
Gao et al (2019) Establishment of porcine and human expanded potential stem cells. Nat Cell Biol 21 687 PMID: 31160711
Shahbazi et al (2017) Pluripotent state transitions coordinate morphogenesis in mouse and human embryos. Nature 552 239 PMID: 29186120
Do you know of a great paper that uses WH-4-023 from Tocris? Please let us know.
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