GSK'872 (GSK2399872A)

Catalog No.S8465

GSK'872 (GSK2399872A) Chemical Structure

Molecular Weight(MW): 383.49

GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.

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Cited by 6 Publications

1 Customer Review

  • (H-K) Cells incubated in the absence or presence of GSK’872, and treated with PM (100 μg/ml) for 24 h. The relative levels of IL6 (H), and IL8 (J) mRNA transcripts were measured by quantitative RT-PCR, and the protein levels of IL6 (I) and IL8 (K) in the culture supernatants, which are in turn were measured by ELISA.

    Cell Physiol Biochem, 2018, 46(2):699-712. GSK'872 (GSK2399872A) purchased from Selleck.

Purity & Quality Control

Choose Selective Serine/threonin kinase Inhibitors

Biological Activity

Description GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
Targets
RIP3K [1]
(Cell-free assay)
1.3 nM
In vitro

When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG MkPWSpVv[3Srb36gZZN{[Xl? NV3aWI5HPSEQvF2= NFvUO|MyKGh? MYTl[oZm[3SrdnXsfUBl\WO{ZXHz[YQhXFB2LX3l[IlifGWmIHP5eI91d3irY3n0fS=> M2HTTVMxPzF5M{C5
U251 NFXpNHdHfW6ldHnvckBie3OjeR?= M17s[FUh|ryP NF\seFgyKGh? M4qwXIVn\mWldHn2[Yx6KGSnY4LlZZNm\CCWUEStcYVlcWG2ZXSgZ5l1d3SxeHnjbZR6 M1ni[FMxPzF5M{C5
HBE cells NX7scWJFTnWwY4Tpc44h[XO|YYm= M1riXVUh|ryP NVHPRpluT1ONJ{i3NkB1emWjdH3lcpQhe2mpbnnmbYNidnSueTDy[YR2[2WmIITo[UBx[XK2aXP1cIF1\SCvYYT0[ZIhMFCPKT3pcoR2[2WmIHX4dJJme3Orb36gc4YhUUx4IHHu[EBKVDhiYYSgZo91cCCvUl7BJIFv\CCycn;0[YlvKGyndnXsdy=> NGHJWWkzQTZ{MUe1Ny=>
K562  MYDGeY5kfGmxbjDhd5NigQ>? NV:zNYR3OSCq NWXS[GtLT1ONJ{i3NkB{cWewaX\pZ4FvfGy7IHnubIljcXSnZDDj[YxtKGSnYYTo Mmr2Nlk2Ojd{MEm=
HT-22 M2L5UWZ2dmO2aX;uJIF{e2G7 NV65c3FuOC5zLDCxJIFv\CBzMPMAje69VQ>? NFT6boQ6KGh? M3zLXZpXSURuIFfTT-KBoTh5MjDhcoQh[2:vYnnuZZRqfmViaX70[ZJ3\W62aX;uJIFtdGW4aXH0[YQhdW:{cHjvcI9ocWNiYXz0[ZJifGmxboOgZY5lKGG2dHXueYF1\WRiY3XscEBl\WG2aDDpcoR2[2WmIHL5JI95gWenbj3ncJVkd3OnIHTldJJqfmG2aX;uJIFv\CC{ZX;4fYdmdmG2aX;u M1PleFI5PzJ2OEmx
MPSC1 cells NWXTOZBbS2WubDD2bYFjcWyrdImgZZN{[Xl? MkHYOkDPxE1? NU\1dGJ{OiCq MVfwdoUufHKnYYTt[Y51KG[xcjCy5qCKcCC5aYToJGdUUyd6N{KgdIFzfGmjbHz5JJJmfmW{c3XkJGNFPDCOLXnu[JVk\WRicnXkeYN1cW:wczDpckBk\WyuII\pZYJqdGm2eR?= NYTXV20xOjZ|MUO5NVU>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Rip1 / Rip3 / p-MLKL / MLKL ; 

PubMed: 31214277     


Hepatocytes were cultured with TNFα (20 ng/mL) for 24 h. Immunoblot analysis of necroptosis markers RIP1, RIP3, and MLKL of hepatocytes pretreated with Nec-1 (100 μM) and GSK′872 (5 μM). 

31214277
Growth inhibition assay
Cell viability; 

PubMed: 24019532     


Viability of 3T3-SA cells at 18 h after treatment with TNF in the presence of Z-VAD-fmk in vehicle control (DMSO) or treated with the indicated concentrations of RIP3 kinase inhibitors, GSK'843 or GSK'872.

24019532
In vivo GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo[3].

Protocol

Cell Research:

[2]

- Collapse
  • Cell lines: 3T3-SA cells
  • Concentrations: 0.3, 1, 3 μM
  • Incubation Time: 18 h
  • Method:

    Viability of 3T3-SA cells at 18 h after treatment with TNF in the presence of Z-VAD-fmk in vehicle control (DMSO) or treated with the indicated concentrations of RIP3 kinase inhibitors, GSK'843 or GSK'872 are assayed.


    (Only for Reference)
Animal Research:

[3]

- Collapse
  • Animal Models: C57BL/6 mice
  • Formulation: dissolved in DMSO (<0.1%) and diluted in saline.
  • Dosages: 1.9 mmol/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (198.17 mM)
Ethanol 40 mg/mL (104.3 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.49
Formula

C19H17N3O2S2

CAS No. 1346546-69-7
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID