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 3 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 M1K1bWZ2dmO2aX;uJIF{e2G7 NUTMdJF2PSEQvF2= MVixJIg> MX\l[oZm[3SrdnXsfUBl\WO{ZXHz[YQhXFB2LX3l[IlifGWmIHP5eI91d3irY3n0fS=> NUj5R2VROzB5MUezNFk>
U251 NFHxXHlHfW6ldHnvckBie3OjeR?= NXvVboh4PSEQvF2= NHfRR2syKGh? MnvY[YZn\WO2aY\lcJkh\GWlcnXhd4VlKFSSND3t[YRq[XSnZDDjfZRwfG:6aXPpeJk> M{CyPFMxPzF5M{C5
HBE cells MkH2SpVv[3Srb36gZZN{[Xl? MV[1JO69VQ>? NYrCfWZQT1ONJ{i3NkB1emWjdH3lcpQhe2mpbnnmbYNidnSueTDy[YR2[2WmIITo[UBx[XK2aXP1cIF1\SCvYYT0[ZIhMFCPKT3pcoR2[2WmIHX4dJJme3Orb36gc4YhUUx4IHHu[EBKVDhiYYSgZo91cCCvUl7BJIFv\CCycn;0[YlvKGyndnXsdy=> MVyyPVYzOTd3Mx?=
K562  M{PqUGZ2dmO2aX;uJIF{e2G7 M1izTFEhcA>? NF;zNplIW0tpOEeyJJNq\26rZnnjZY51dHliaX7obYJqfGWmIHPlcIwh\GWjdHi= MlrFNlk2Ojd{MEm=
HT-22 NIGxVJlHfW6ldHnvckBie3OjeR?= NEWwVmQxNjFuIEGgZY5lKDFy4pEJ{txO MV25JIg> M1n1UppXSURuIFfTT-KBoTh5MjDhcoQh[2:vYnnuZZRqfmViaX70[ZJ3\W62aX;uJIFtdGW4aXH0[YQhdW:{cHjvcI9ocWNiYXz0[ZJifGmxboOgZY5lKGG2dHXueYF1\WRiY3XscEBl\WG2aDDpcoR2[2WmIHL5JI95gWenbj3ncJVkd3OnIHTldJJqfmG2aX;uJIFv\CC{ZX;4fYdmdmG2aX;u MWiyPFczPDh7MR?=
MPSC1 cells NVTnZWZ[S2WubDD2bYFjcWyrdImgZZN{[Xl? MXe2JO69VQ>? MX6yJIg> NWnhTW1zeHKnLYTy[YF1dWWwdDDmc5IhOuLCiXige4l1cCCJU1unPFczKHCjcoTpZYxtgSC{ZY\ldpNm\CCFRESwUE1qdmS3Y3XkJJJm\HWldHnvcpMhcW5iY3XscEB3cWGkaXzpeJk> MlLUNlY{OTN7MUW=

... Click to View More Cell Line Experimental Data

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

Protocol

Cell Research:

[2]

+ Expand
  • 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]

+ Expand
  • 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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Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID