1. Apoptosis
  2. RIP kinase
  3. GSK-872

GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.

For research use only. We do not sell to patients.

GSK-872 Chemical Structure

GSK-872 Chemical Structure

CAS No. : 1346546-69-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 250 In-stock
50 mg USD 390 In-stock
100 mg USD 600 In-stock
200 mg   Get quote  
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Customer Review

Based on 61 publication(s) in Google Scholar

Other Forms of GSK-872:

Top Publications Citing Use of Products

58 Publications Citing Use of MCE GSK-872

WB

    GSK-872 purchased from MedChemExpress. Usage Cited in: Transl Stroke Res. 2021 Dec;12(6):991-1017.  [Abstract]

    Delayed administration of GSK-872 reduces the protein level of RIP3K or MLKL and GFAP after OGD/Re injury. Astrocytes are exposed to OGD for 6 h followed by reoxygenation for 24 h. GSK-872 (10 μM) is added to the cells upon reoxygenation.

    GSK-872 purchased from MedChemExpress. Usage Cited in: J Immunol. 2018 Apr 15;200(8):2826-2834.  [Abstract]

    Wild-type BMDMs are treated with or without PM (20 μg/ml), and DMSO, Necrostatin-1 (10 μM), and GSK’872 (5 μM) as indicated, the expression of p-IkBα and p-RELA are measured by Western blot.

    GSK-872 purchased from MedChemExpress. Usage Cited in: Chin J of Oncol Prev and Treat. 2018, 10(2): 105-109.

    In the inhibitor group,GSK'872 is injected intrathecally at 30 min before model establishment; in the saline group,the same volume of saline is intrathecally injected.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury[1][2][3].

    IC50 & Target

    RIPK3

     

    In Vitro

    GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner[1].

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

    Cell Viability Assay[1]

    Cell Line: HT-29 cells
    Concentration: 0.01, 0.03 , 0.1, 0.3, 1, and 3 μM
    Incubation Time: 24 hours
    Result: Blocked TNF-induced necroptosis in a concentration-dependent manner.
    In Vivo

    GSK-872 (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein[3].

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

    Animal Model: Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)[3]
    Dosage: 25 mM/6 μL
    Administration: Syringe pump (intracerebroventricular) at 30 min after SAH
    Result: Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.
    Molecular Weight

    383.49

    Formula

    C19H17N3O2S2

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=S(C1=CC=C2N=CC=C(C2=C1)NC3=CC=C4SC=NC4=C3)(C(C)C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (260.76 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 2.6076 mL 13.0381 mL 26.0763 mL
    5 mM 0.5215 mL 2.6076 mL 5.2153 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.52 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 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 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.52 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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.91%

    References

    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 2.6076 mL 13.0381 mL 26.0763 mL 65.1907 mL
    5 mM 0.5215 mL 2.6076 mL 5.2153 mL 13.0381 mL
    10 mM 0.2608 mL 1.3038 mL 2.6076 mL 6.5191 mL
    15 mM 0.1738 mL 0.8692 mL 1.7384 mL 4.3460 mL
    20 mM 0.1304 mL 0.6519 mL 1.3038 mL 3.2595 mL
    25 mM 0.1043 mL 0.5215 mL 1.0431 mL 2.6076 mL
    30 mM 0.0869 mL 0.4346 mL 0.8692 mL 2.1730 mL
    40 mM 0.0652 mL 0.3260 mL 0.6519 mL 1.6298 mL
    50 mM 0.0522 mL 0.2608 mL 0.5215 mL 1.3038 mL
    60 mM 0.0435 mL 0.2173 mL 0.4346 mL 1.0865 mL
    80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8149 mL
    100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6519 mL
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    GSK-872 Related Classifications

    Help & FAQs
    • 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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    Product Name:
    GSK-872
    Cat. No.:
    HY-101872
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