GSK 2830371
Tocris Bioscience, part of Bio-Techne | Catalog # 5140
Potent and selective allosteric inhibitor of Wip1 phosphatase
Key Product Details
Description
Potent and selective allosteric inhibitor of Wip1 phosphatase
Product Description
GSK 2830371 is a 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. Potentiates growth inhibitory effects of MDM2 inhibition in cancer cell lines in a p53-dependent manner. Orally bioavailable.Licensing Information
Sold for research purposes only under agreement from GlaxoSmithKlineProduct Specifications
Molecular Weight
461.02
Formula
C23H29ClN4O2S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.1 | 100 | |
| Ethanol | 23.05 | 50 |
Preparing Stock Solutions
for GSK 2830371
The following data is based on the product molecular weight 461.02
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Esfandiari Chemical inhibition of wild-type p53-induced phosphatase 1 (WIP1/PPM1D) by GSK2830371 potentiates the sensitivity to MDM2 inhibitors in a p53-dependent manner. Mol.Cancer Ther. 2016 PMID: 26832796
- Gilmartin Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 2014 PMID: 24390428
Product Specific Notices for GSK 2830371
For research use only
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