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

GSK-872 hydrochloride 

Cat. No.: HY-101872A Purity: 99.64%
Handling Instructions

GSK-872 hydrochloride 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 hydrochloride 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 hydrochloride Chemical Structure

GSK-872 hydrochloride Chemical Structure

CAS No. : 2703752-81-0

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10 mM * 1 mL in DMSO USD 99 In-stock
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25 mg USD 330 In-stock
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100 mg USD 920 In-stock
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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of GSK-872 hydrochloride:

Top Publications Citing Use of Products

    GSK-872 hydrochloride purchased from MCE. Usage Cited in: J Immunol. 2018 Apr 15;200(8):2826-2834.

    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 hydrochloride purchased from MCE. 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.

    GSK-872 hydrochloride purchased from MCE. Usage Cited in: Transl Stroke Res. 2021 Dec;12(6):991-1017.

    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.
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    Description

    GSK-872 hydrochloride 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 hydrochloride 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

    IC50: 1.3 nM (RIPK3)[1]

    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].

    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 hydrochloride (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 hydrochloride can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein[3].

    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

    419.95

    Formula

    C₁₉H₁₈ClN₃O₂S₂

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (23.81 mM; ultrasonic and warming and heat to 60°C)

    H2O : 2.5 mg/mL (5.95 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3812 mL 11.9062 mL 23.8124 mL
    5 mM 0.4762 mL 2.3812 mL 4.7625 mL
    10 mM 0.2381 mL 1.1906 mL 2.3812 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.21 mg/mL (0.50 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Product Name:
    GSK-872 hydrochloride
    Cat. No.:
    HY-101872A
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