An inhibitor of Wip1 phosphatase
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GSK2830371

Item No. 16973

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide
CAS Number
1404456-53-6
Molecular Formula
C23H29ClN4O2S
Formula Weight
461.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:5): 0.1 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/ml
λmax
229, 255 nm
SMILES
ClC1=CC(NCC2=CC=C(C(N[C@H](C(NC3CC3)=O)CC4CCCC4)=O)S2)=C(C)N=C1
InChi Code
InChI=1S/C23H29ClN4O2S/c1-14-19(11-16(24)12-25-14)26-13-18-8-9-21(31-18)23(30)28-20(10-15-4-2-3-5-15)22(29)27-17-6-7-17/h8-9,11-12,15,17,20,26H,2-7,10,13H2,1H3,(H,27,29)(H,28,30)/t20-/m0/s1
InChi Key
IVDUVEGCMXCMSO-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $203

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    25 mg

    $420

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    Cayman Chemical
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    Product Description

    GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM).1 It displays selectivity for Wip1 over 21 other phosphatases.1 GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53.1 This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gilmartin, A.G., Faitg, T.H., Richter, M., et al. Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat. Chem. Biol. 10(3), 181-187 (2014).