GSK 2830371
Based on 13 publication(s) in Google Scholar
GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 1404456-53-6
- Formula: C23H29ClN4O2S
- Molecular Weight:461.02
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Phosphatase Inhibitor Library
HY-L081
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) GSK 2830371
More- Nat Commun. 2022 Feb 1;13(1):604. [Abstract]
- Nat Commun. 2018 Sep 25;9(1):3923. [Abstract]
- Nucleic Acids Res. 2023 Feb 22;51(3):1154-1172. [Abstract]
- Cell Death Dis. 2019 Oct 28;10(11):818. [Abstract]
- Oncogene. 2024 Oct;43(42):3081-3093. [Abstract]
- Mol Oncol. 2024 Jan;18(1):6-20. [Abstract]
- FEBS J. 2021 Oct;288(20):6035-6051. [Abstract]
- Reprod Biomed Online. 2021 Aug;43(2):161-171. [Abstract]
- Reprod Fertil Dev. 2020 Dec;32(18):1350-1356. [Abstract]
- bioRxiv. 2026 Jan 24.
- Research Square Preprint. 2021 Aug.
- University Medical Center Utrecht. 2018.
- Oncotarget. 2016 Mar 22;7(12):14458-75. [Abstract]
Customer Validation & Images
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WB
Biological Activity
IC50: 6 nM (Wip1 phosphatase)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
9.5 μM
Compound: GSK2830371
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Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs
Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs
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[PMID: 26358280] |
| Sf9 | IC50 |
0.006 μM
Compound: 31; GSK2830371
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Inhibition of N-terminal FLAG-His8-tagged human Wip1 (2 to 420 residues) expressed in bac-to-bac baculovirus expression system infected Sf9 cells
Inhibition of N-terminal FLAG-His8-tagged human Wip1 (2 to 420 residues) expressed in bac-to-bac baculovirus expression system infected Sf9 cells
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[PMID: 38197367] |
| Sf9 | IC50 |
6 nM
Compound: 8; GSK2830371
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Inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus-infected insect SF9 cells assessed as fluorescein diphosphate hydrolysis after 5 mins by fluorescence assay
Inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus-infected insect SF9 cells assessed as fluorescein diphosphate hydrolysis after 5 mins by fluorescence assay
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[PMID: 26914744] |
GSK 2830371 potently inhibits Wip1 (2-420) dephosphorylation of FDP and the endogenous substrates phospho-p38 MAPK (T180) with IC50 values of 6 nM and 13 nM, respectively. In the PPM1D-amplified MCF7 breast carcinoma cells, treatment with GSK 2830371 (0.04, 0.11, 0.33, 1, 3, and 9 μM) increased phosphorylation of substrates in a concentration-dependent manner. Treatment of MX-1 and MCF7 cells (Wip1amplified, p53 wild type) with GSK 2830371 (0.001, 0.01, 0.1, 1, and 10 μM) causes concentration-dependent effects in cell growth assays[1]. GSK2830371 has a 50% growth inhibitory concentration (GI50) of 2.65 μM±0.54 (SEM) in MCF-7 cells. Treatment of MCF-7 cells with 2.5μM GSK2830371 results in marked time-dependent degradation of both isoforms of WIP1 over 8 hours which correlated with p53 stabilisation and phospho-p53Ser15 (pp53Ser15)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1404456-53-6
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Appearance Solid
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Molecular Weight 461.02
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Formula C23H29ClN4O2S
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Color White to light yellow
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SMILES
ClC1=CN=C(C)C(NCC2=CC=C(C(N[C@@H](CC3CCCC3)C(NC4CC4)=O)=O)S2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
2022 Feb 1;13(1):604. PMID: 35105861 -
Nat Commun
2018 Sep 25;9(1):3923. PMID: 30254262 -
Nucleic Acids Res
Phosphorylation of TRF2 promotes its interaction with TIN2 and regulates DNA damage response at telomeres. [Abstract]2023 Feb 22;51(3):1154-1172. PMID: 36651296 -
Cell Death Dis
Truncated PPM1D impairs stem cell response to genotoxic stress and promotes growth of APC-deficient tumors in the mouse colon. [Abstract]2019 Oct 28;10(11):818. PMID: 31659152 -
Oncogene
2024 Oct;43(42):3081-3093. PMID: 39237765 -
Mol Oncol
2024 Jan;18(1):6-20. PMID: 37067201 -
FEBS J
2021 Oct;288(20):6035-6051. PMID: 33982878 -
Reprod Biomed Online
2021 Aug;43(2):161-171. PMID: 34210610 -
Reprod Fertil Dev
Wild-type p53-induced phosphatase 1 (WIP1) regulates the proliferation of swine Sertoli cells through P53. [Abstract]2020 Dec;32(18):1350-1356. PMID: 33287951 -
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Oncotarget
Inhibition of WIP1 phosphatase sensitizes breast cancer cells to genotoxic stress and to MDM2 antagonist nutlin-3. [Abstract]2016 Mar 22;7(12):14458-75. PMID: 26883108
GSK 2830371 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Mar 22;7(12):14458-75. [Abstract]
Immunoblot analysis of MCF7 cells reveals that addition of GSK2830371 results in a rapid phosphorylation of p53 at Ser15. Two days after addition of GSK2830371, MCF7 cells show increased levels of p21 which indicates a strong activation of the p53 pathway.
Solvent & Solubility
DMSO : 100 mg/mL (216.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The primary in vitro Wip1 enzymatic assay measured fluorescence generated by Wip-1 (2-420) hydrolysis of fluorescein diphosphate (FDP). 50 μM FDP substrate is added with GSK 2830371 or DMSO at room temperature before addition of 10 nM Wip1 in assay buffer (50 mM TRIS, pH 7.5, 30 mM MgCl2, 0.8 mM CHAPS, 0.05 mg/mL BSA). Fluorescent signal is detected on a Spectramax microplate reader (485/530 nm)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells are seeded into 96 well plates at 200-400 cells per well and treated with GSK 2830371 dilution series on day 1. After 7 d, we used the CellTiter-Glo cell viability assay to determine effects on cell growth. Luminescent signal is detected on an EnVision 2104. For clonogenic assays, cells are seeded in 12-well tissue culture plates at 2,000 cells per well. Cells are treated with a compound dilution series on day 1 and again on day 7. After 14 d, cells are washed with 1× PBS, stained with 1 mL of Coomassie Brilliant Blue R-250, and colonies are quantitated with the Optomax Sorcerer colony counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female SCID mice are subcutaneously inoculated with 1×107 DOHH2 cells and tumor growth is monitored with electronic calipers. When tumors reached 100-200 mm3, animals are treated orally twice (BID) or thrice (TID) daily with vehicle (2% DMSO and 40% Captisol, pH 4.0) or GSK 2830371. For efficacy studies, eight mice per group are administered with GSK 2830371 at 75 or 150 mg per kg body weight BID or 150 mg per kg body weight TID. Tumor growth inhibition (% difference in tumor growth compared to control) is calculated when tumors for vehicle-control mice exceeded 1,000 mm3 (day 11). For pharmacodynamic biomarker analysis, DOHH2 tumors from three mice are harvested 2 or 4 h after final dose following 14 d of treatment with either vehicle or GSK 2830371 at 75 or 150 mg per kg body weight, BID; tumors are frozen in liquid nitrogen for subsequent lysis and western blot analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Gilmartin AG, et al. Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat Chem Biol. 2014 Mar;10(3):181-7. [Content Brief]
[2]. Esfandiari A, et al. 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 Mar;15(3):379-91. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1691 mL | 10.8455 mL | 21.6910 mL | 54.2276 mL |
| 5 mM | 0.4338 mL | 2.1691 mL | 4.3382 mL | 10.8455 mL | |
| 10 mM | 0.2169 mL | 1.0846 mL | 2.1691 mL | 5.4228 mL | |
| 15 mM | 0.1446 mL | 0.7230 mL | 1.4461 mL | 3.6152 mL | |
| 20 mM | 0.1085 mL | 0.5423 mL | 1.0846 mL | 2.7114 mL | |
| 25 mM | 0.0868 mL | 0.4338 mL | 0.8676 mL | 2.1691 mL | |
| 30 mM | 0.0723 mL | 0.3615 mL | 0.7230 mL | 1.8076 mL | |
| 40 mM | 0.0542 mL | 0.2711 mL | 0.5423 mL | 1.3557 mL | |
| 50 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | 1.0846 mL | |
| 60 mM | 0.0362 mL | 0.1808 mL | 0.3615 mL | 0.9038 mL | |
| 80 mM | 0.0271 mL | 0.1356 mL | 0.2711 mL | 0.6778 mL | |
| 100 mM | 0.0217 mL | 0.1085 mL | 0.2169 mL | 0.5423 mL |
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