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

GSK-872 

Cat. No.: HY-101872 Purity: 99.86%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 330 In-stock
50 mg USD 590 In-stock
100 mg USD 920 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 48 publication(s) in Google Scholar

Other Forms of GSK-872:

Top Publications Citing Use of Products

45 Publications Citing Use of MCE GSK-872

WB

    GSK-872 purchased from MCE. 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 MCE. 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 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.

    • 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

    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 (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].

    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

    Appearance

    Solid

    Formula

    C19H17N3O2S2
    CAS No.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (260.76 mM; Need ultrasonic)

    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
    10 mM 0.2608 mL 1.3038 mL 2.6076 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.91%

    COA (251 KB) LCMS (134 KB)

    Handling Instructions (2659 KB)
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    GSK-8721346546-69-7GSK872GSK 872RIP kinaseReceptor-interacting protein kinasesRIPKcytoplasmictranslocationHMGB1brainedemaneurologicaldeficitsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email address *

    Phone number *

    		 

    Organization name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GSK-872
    Cat. No.:
    HY-101872
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email address *

    Phone number

    		 

    Department *

    Organization name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.