Biological Activity
Potent and selective allosteric inhibitor of Wip1 phosphatase (IC50 = 6 nM). Exhibits selectivity for Wip1 over 21 other phosphatases. Increases phosphorylation of Wip1 substrates, including p53, Chk2, H2AX and ATM. Attenuates tumor cell growth in a variety of lymphoid cell lines. Also inhibits lymphoma xenograft growth in vivo. Orally bioavailable.
Licensing Information
Sold for research purposes only under agreement from GlaxoSmithKline
Compound Libraries
GSK 2830371 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 461.02 |
| Formula | C23H29ClN4O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1404456-53-6 |
| PubChem ID | 70983932 |
| InChI Key | IVDUVEGCMXCMSO-FQEVSTJZSA-N |
| Smiles | ClC1=CC(NCC2=CC=C(C(N[C@H]([C@@](NC4CC4)=O)CC3CCCC3)=O)S2)=C(C)N=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 | 46.1 | 100 | |
| ethanol | 23.05 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 461.02. 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 | 2.17 mL | 10.85 mL | 21.69 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.34 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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References
References are publications that support the products' biological activity.
Gilmartin et al (2014) Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 10 181 PMID: 24390428
Keywords: GSK 2830371, supplier, GSK2830371, potent, selective, allosteric, inhibitors, inhibits, wip1, phosphatases, antitumor, orally, bioavailable, Protein, Ser/Thr, Phosphatases, Protein, Ser/Thr, Phosphatases, Tocris Bioscience
