GSK 2830371

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Cat.No. 5140 - GSK 2830371 | C23H29ClN4O2S | CAS No. 1404456-53-6
Description: Potent and selective allosteric inhibitor of Wip1 phosphatase
Chemical Name: 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

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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Product Datasheets

Safety Datasheet

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


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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

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Cancer

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