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Chemical Structure| 1346546-69-7 Chemical Structure| 1346546-69-7

Structure of GSK-872
CAS No.: 1346546-69-7

Chemical Structure| 1346546-69-7

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GSK'872 is an inhibitor of RIPK3 with IC50 of 1.8 nM and kinase activity (IC50 = 1.3 nM). It also exhibits supression of necrosis induced by toll-like receptor 3.

Synonyms: GSK2399872A; GSK'872

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Product Details of GSK-872

CAS No. :1346546-69-7
Formula : C19H17N3O2S2
M.W : 383.49
SMILES Code : O=S(C1=CC=C2N=CC=C(NC3=CC=C(SC=N4)C4=C3)C2=C1)(C(C)C)=O
Synonyms :
GSK2399872A; GSK'872
MDL No. :MFCD30481302
InChI Key :ZCDBTQNFAPKACC-UHFFFAOYSA-N
Pubchem ID :54674134

Safety of GSK-872

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
hepG2 cells 5 μM 24 h GSK-872 can restore cell death caused by knockdown of HABON Cell Death Discov. 2022 Apr 6;8(1):171.
hNPCs 5 μM To study the mechanism of ZIKV-induced cell death, GSK872 was used to inhibit necroptosis Cells. 2020 Nov 16;9(11):2487.
SMMC-7721 cells 5 μM 24 h GSK-872 can restore cell death caused by knockdown of HABON Cell Death Discov. 2022 Apr 6;8(1):171.
Huh7 cells 5 μM 24 h GSK-872 can restore cell death caused by knockdown of HABON Cell Death Discov. 2022 Apr 6;8(1):171.
T24 resistant cells 2 µM 24 h Inhibited RIP3 phosphorylation and reduced cell death caused by shikonin or its combination with cisplatin Int J Biol Sci. 2018 Oct 20;14(13):1883-1891.
RAW264.7 cells 5 µM Inhibition of RIPK3 kinase activity reduced the accumulation of autophagic flux Clin Transl Med. 2023 Jul;13(7):e1334.
NZM2328 mouse podocyte cell line 3µM 1 h GSK872 inhibited the phosphorylation of RIP3 and MLKL, and blocked the activation of the NLRP3 inflammasome J Autoimmun. 2019 Sep;103:102286.
RAW264.7 cells 3 µM 24 h GSK872 inhibited the RIP3 signaling pathway, reduced the expression of inflammatory cytokines and chemokines, and significantly decreased the apoptosis rate of RAW264.7 cells. Front Immunol. 2021 Mar 25;12:624360.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Sepsis model Intraperitoneal injection 3 mg/kg Administered at 0, 12, 24, 48, and 72 hours post-CLP Inhibition of necroptotic signaling ameliorated sepsis-induced multiple organ dysfunction and systemic inflammation Clin Transl Med. 2023 Jul;13(7):e1334.
Mouse MRL/lpr mice Intraperitoneal injection 1mg/kg Once daily for 2 weeks GSK872 significantly reduced the expression of p-RIP3 and p-MLKL in the kidneys, inhibited the activation of the NLRP3 inflammasome, and improved nephritis symptoms J Autoimmun. 2019 Sep;103:102286.
Mice LPS-induced systemic inflammation model Intraperitoneal injection 2 mg/kg Single dose, lasting 72 hours GSK872 suppressed RIP3-mediated necroptosis and restored Kir4.1 protein expression, alleviating LPS-induced brain endothelial cell damage and increased neuronal excitability. J Neuroinflammation. 2022 Feb 2;19(1):29
Mice DSS-Con A induced autoimmune hepatitis model Intraperitoneal injection 1 mg/kg Single dose, lasting 1 hour GSK872 significantly inhibited the activation of the RIP3 signaling pathway, reduced the activation and infiltration of liver macrophages, and alleviated liver inflammation and injury. Front Immunol. 2021 Mar 25;12:624360.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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