GSK 2830371

Name: GSK 2830371
Brand: MedChemExpress
SKU: HY-15832
Rating: 5.0 (13 reviews)

Cat. No.: HY-15832 Pureté: 99.75%: Fiche technique
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GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC₅₀ of 6 nM.

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CAS No. : 1404456-53-6

Size	Stock	Quantité

Échantillon gratuit (0.1 - 0.2 mg)	Appliquer maintenant
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	En stock	Estimated Time of Arrival: December 31
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Based on 13 publication(s) in Google Scholar

Other Forms of GSK 2830371:

(R)-GSK 2830371 In-stock

13 Publications Citing Use of MCE GSK 2830371

: 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.

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Description

GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC₅₀ of 6 nM.

IC₅₀ & Target

IC50: 6 nM (Wip1 phosphatase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	6 1 Compound: 8; GSK2830371	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	[PMID: 26914744]
MCF7	IC₅₀	9.5 3 Compound: GSK2830371	Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs	[PMID: 26358280]
Sf9	IC₅₀	6 1 Compound: 8; GSK2830371	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	[PMID: 26914744]
MCF7	IC₅₀	9.5 3 Compound: GSK2830371	Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs	[PMID: 26358280]
MCF7	IC₅₀	9.5 3 Compound: GSK2830371	Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs	[PMID: 26358280]
Sf9	IC₅₀	0.006 3 Compound: 31; GSK2830371	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	[PMID: 38197367]
Sf9	IC₅₀	0.006 3 Compound: 31; GSK2830371	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	[PMID: 38197367]
Sf9	IC₅₀	6 1 Compound: 8; GSK2830371	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	[PMID: 26914744]

In Vitro

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-p53^Ser15 (pp53^Ser15)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In a pharmacodynamic assay, orally administered GSK 2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreased Wip1protein concentrations in DOHH2 tumors. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK 2830371 inhibits the growth of DOHH2 tumor xenografts by 41% and 68%, respectively. Comparable tumor growth inhibition is observed in mice treated BID with either 75 or 150 mg per kg body weight. Greater tumor growth inhibition with the TID schedule is consistent with a short half-life of GSK 2830371 in mice and suggests that sustained inhibition of Wip1 may be required for maximal antitumor effect^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Masse moléculaire

461.02

Formule

C₂₃H₂₉ClN₄O₂S

CAS No.

1404456-53-6

Appearance

Solid

Color

White to light yellow

SMILES

ClC1=CN=C(C)C(NCC2=CC=C(C(N[C@@H](CC3CCCC3)C(NC4CC4)=O)=O)S2)=C1

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1691 mL	10.8455 mL	21.6910 mL
5 mM	0.4338 mL	2.1691 mL	4.3382 mL
10 mM	0.2169 mL	1.0846 mL	2.1691 mL

View the 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.

Calculateur de molarité
Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Pureté et documentation

Purity: 99.79%

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Fiche technique (281 KB) SDS (393 KB)

COA (251 KB) RP-HPLC (223 KB) MS (70 KB)

Instruction de manipulation (2659 KB)

Références

[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]

Essai de kinase ^[1]	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]. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Test cellulaire ^[1]	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]. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale ^[1]	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. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références	[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

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

GSK 2830371 Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GSK 28303711404456-53-6GSK2830371GSK-2830371PhosphataseInhibitorinhibitorinhibit

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GSK 2830371

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Other Forms of GSK 2830371:

GSK 2830371 Related Antibodies

13 Publications Citing Use of MCE GSK 2830371

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Activité biologique

Protocole

Pureté et documentation

Références

Avis client

GSK 2830371 Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

GSK 2830371 Related Classifications

Keywords:

Vos produits récemment consultés:

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