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GSK 2830371

Cat. No. 5140 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective allosteric inhibitor of Wip1 phosphatase
化学名： 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for GSK 2830371

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.

许可信息

Sold for research purposes only under agreement from GlaxoSmithKline

化合物库 for GSK 2830371

GSK 2830371 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。

技术数据 for GSK 2830371

分子量 461.02
公式 C23H29ClN4O2S
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for GSK 2830371

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.1 100
ethanol 23.05 50

制备储备液 for GSK 2830371

以下数据基于产品分子量 461.02。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for GSK 2830371

参考文献是支持产品生物活性的出版物。

Gilmartin et al (2014) Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 10 181 PMID: 24390428

Esfandiari et al (2016) 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. 15 379 PMID: 26832796

If you know of a relevant reference for GSK 2830371, please let us know.

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关键词: GSK 2830371, GSK 2830371 supplier, GSK2830371, potent, selective, allosteric, inhibitors, inhibits, wip1, phosphatases, antitumor, orally, bioavailable, Protein, Ser/Thr, Phosphatases, 5140, Tocris Bioscience

1 篇 GSK 2830371 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GSK 2830371 的部分引用包括：

Griffith D et al (2018) Parainfluenza Virus Infection Sensitizes Cancer Cells to DNA-Damaging Agents: Implications for Oncolytic Virus Therapy. J Virol 92 PMID: 29343567

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